☆ 4.6 Review

Six-membered Aromatic Nitrogen Heterocyclic Anti-Tumor Agents: Synthesis and Applications

CHEMICAL RECORD (2023)

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Review Chemistry, Medicinal

Quinoline: Synthesis to Application

Ravi Kumar Mittal et al.

Summary: This review provides a comprehensive report on the synthesis, reactivity, and therapeutic values of the quinoline ring. The reactivity of quinoline with metal, electrophile, and other reactive counterparts shapes the quinoline pharmacophore, which is an important part of this report. The spectroscopic characteristics of quinoline are also discussed with suitable illustrations. Additionally, the synthesis of quinoline and its derivatives, along with the new developments in catalytic systems, are presented, and the relevant information is summarized under various activity classes. The synthetic parameters of quinoline with regard to important pharmacological aspects are highlighted.

MEDICINAL CHEMISTRY (2023)

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Review Chemistry, Medicinal

Pyrimidine derivatives with antitubercular activity

Vladimir Finger et al.

Summary: This review provides an overview of recent advances in the hit-to-lead drug discovery studies of pyrimidine-containing compounds with antitubercular activity, focusing on their structural diversity. The review discusses the targets and structure-activity relationships of different pyrimidine families in the first part and categorizes unexplored or speculative targets of antitubercular pyrimidine derivatives based on their structural types in the second part.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)

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Review Biochemistry & Molecular Biology

Cabozantinib, Vandetanib, Pralsetinib and Selpercatinib as Treatment for Progressed Medullary Thyroid Cancer with a Main Focus on Hypertension as Adverse Effect

Linnea Hojer Wang et al.

Summary: This manuscript investigates four tyrosine kinase inhibitors (TKIs), cabozantinib, vandetanib, pralsetinib, and selpercatinib, used for treating advanced and/or metastatic medullary thyroid cancer (MTC). The focus is on treatment-related hypertension, a well-known adverse effect (AE) of these TKIs. While TKI-induced hypertension is rarely a dose-limiting side effect, complications associated with hypertension can increase with longer patient survival without proper medication.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

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Review Biochemistry & Molecular Biology

Treatment of Advanced Non-Small Cell Lung Cancer with RET Fusions: Reality and Hopes

Danilo Rocco et al.

Summary: RET-selective tyrosine kinase inhibitors (TKIs) selpercatinib and pralsetinib have transformed the treatment landscape for RET-positive (RET+) advanced non-small cell lung cancer (NSCLC) due to their effectiveness and safety profiles. However, there is still limited understanding of resistance mechanisms after treatment with these TKIs. Chemotherapy +/- immunotherapy is currently recommended as a second-line treatment for patients progressing on selpercatinib or pralsetinib. Therefore, further research on the resistance mechanisms triggered by RET-TKIs is crucial.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

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Article Veterinary Sciences

Immunohistochemical analysis of expression of VEGFR2, KIT, PDGFR-β, and CDK4 in canine urothelial carcinoma

Laura C. Setyo et al.

Summary: This study found that tyrosine kinases, including VEGFR2 and PDGFR-beta, are present in canine urothelial carcinomas (UCs). The expression of CDK4 in UC cells is weaker compared to normal and cystitis bladder samples. The overexpression of VEGFR2 suggests that it may serve as a potential therapeutic target in UC.

JOURNAL OF VETERINARY DIAGNOSTIC INVESTIGATION (2023)

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Review Chemistry, Medicinal

An Explicative Review on the Progress of Quinazoline Scaffold as Bioactive Agents in the Past Decade

Naman Jain et al.

Summary: In the past decade, quinazoline has been extensively explored by researchers worldwide in medicinal chemistry. Its unique structural features offer a wide range of possibilities for substitutions involving nitrogen and carbonyl groups. In the current COVID-19 situation, hydroxychloroquine, a quinoline-based antimalarial drug, has been used for the treatment of severe infections. Various substitution patterns, hybrids, and conjugates of quinazoline have been developed and studied for their pharmacological activities, including anticancer, anti-inflammatory, antimalarial, antitubercular, and more. The scaffold shows potential for various pharmacological activities, particularly antimicrobial and anti-hypertensive effects. This review article aims to examine the physicochemical properties, chemistry, and pharmacological profile of quinazoline.

MEDICINAL CHEMISTRY (2023)

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Article Oncology

Osimertinib and Selpercatinib Efficacy, Safety, and Resistance in a Multicenter, Prospectively Treated Cohort of EGFR-Mutant and RET Fusion-Positive Lung Cancers

Julia Rotow et al.

Summary: This study found that the combination of osimertinib and selpercatinib can be effective in treating EGFR-mutant NSCLC with acquired RET fusions as a mechanism of EGFR inhibitor resistance. It supports the need for further evaluation of this combination therapy in prospective studies.

CLINICAL CANCER RESEARCH (2023)

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Review Chemistry, Organic

An Insight on the Prospect of Quinazoline and Quinazolinone Derivatives as Anti-tubercular Agents

Namrata Kushwaha et al.

Summary: Multiple drugs based on heterocyclic molecules have been developed for treating various symptoms. Quinazoline and quinazolinone derivatives exhibit extensive pharmacological and biological characteristics, including their potency as anti-tubercular agents. This review summarizes the reported anti-tubercular drugs designed using quinazoline and quinazolinone derivatives.

CURRENT ORGANIC SYNTHESIS (2023)

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Review Pharmacology & Pharmacy

Targeting the EGFR signaling pathway in cancer therapy: What's new in 2023?

Sushanta Halder et al.

Summary: This review discusses the importance of epidermal growth factor receptor (EGFR) in multiple cancers and its role in cellular processes. It also highlights the newly identified pathways, resistance mechanisms, and adverse effects of EGFR inhibitors. The latest research on EGFR/panEGFR inhibitors and the potential of combining them with immune checkpoint inhibitors are summarized. Suggestions for developing specific compounds to target mutations and reducing adverse events are provided.

EXPERT OPINION ON THERAPEUTIC TARGETS (2023)

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Review Chemistry, Multidisciplinary

Microwave irradiation for the synthesis of quinoline scaffolds: a review

Manesh S. Tople et al.

Summary: This review provides a detailed overview of microwave-assisted synthesis of quinoline and its derivatives. The importance of environmentally friendly synthesis methods is emphasized, and the results show that microwave irradiation synthesis is more efficient than traditional methods. These techniques have the advantages of pollution-free, energy-efficient, and time-saving, and can be applied in industrial production.

JOURNAL OF THE IRANIAN CHEMICAL SOCIETY (2023)

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Review Oncology

Gefitinib: An Updated Review of its Role in the Cancer Management, its Nanotechnological Interventions, Recent Patents and Clinical Trials

Pankaj Kumar et al.

Summary: This review summarizes the journey of gefitinib as an established anticancer drug for the management of various cancers. The mechanism of action, established anticancer activities, combination therapy, nanoformulations, as well as recent clinical trials and patents on gefitinib are discussed. Data for this review was collected from scientific databases and recent pre-clinical and clinical studies demonstrating the efficacy of gefitinib were summarized. The review concludes that gefitinib has significant advantages and the use of nanotechnology addresses associated biopharmaceutical problems. Combination therapy using gefitinib and various anticancer molecules shows an improved anticancer profile.

RECENT PATENTS ON ANTI-CANCER DRUG DISCOVERY (2023)

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Review Chemistry, Medicinal

Quinoline-based Anti-oncogenic Molecules: Synthesis and Biological Evaluation

Shivangi Sharma et al.

Summary: This article discusses the presence of quinoline and its analogues in various natural products, many of which have significant bioactivities as pharmacophores. It specifically focuses on the anti-cancer properties of quinoline derivatives and their analogues, providing valuable insights for the scientific community. Additionally, the article reveals the synthetic aspect of these anti-cancer quinoline derivatives, which can be synthesized using acids, bases, azides, and reagents such as Jone's reagent and Lawesson's reagent.

MEDICINAL CHEMISTRY (2023)

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Review Chemistry, Medicinal

Harnessing the necessary nitrogen atom in chemical biology and drug discovery

Lewis D. Pennington et al.

Summary: Replacing an aromatic methine group with a nitrogen atom can significantly improve various pharmacological parameters and enhance the efficiency of multiparameter optimization efforts in small molecule drug discovery.

MEDICINAL CHEMISTRY RESEARCH (2023)

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Review Oncology

RET Fusion-Positive Non-small Cell Lung Cancer: The Evolving Treatment Landscape

Silvia Novello et al.

Summary: This narrative review aims to summarize the efficacy and safety of available therapies for RET fusion-positive non-small cell lung cancer (NSCLC) and central nervous system (CNS) metastases. It provides background information on RET rearrangements in NSCLC and molecular testing options, along with an overview of clinical guidelines for broad molecular testing. The review discusses the efficacy and safety of potential treatments, including multikinase inhibitors, RET-selective inhibitors, pemetrexed-based therapy, and immunotherapies, and highlights RET-selective inhibitors as preferred first-line therapy options for RET fusion-positive metastatic NSCLC.

ONCOLOGIST (2023)

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Review Chemistry, Multidisciplinary

Synthesis and Antiviral Efficacy of Pyrimidine Analogs Targeting Viral Pathways

N. Jeelan Basha et al.

Summary: Viruses can cause chronic to acute pathogenesis, and antiviral drugs have been used for decades to treat infections caused by these pathogens. However, finding a molecule that can effectively eliminate or control viral infection without inducing resistance is a challenge.

CHEMISTRYSELECT (2023)

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Article Oncology

Combination Therapies with CDK4/6 Inhibitors to Treat KRAS-Mutant Pancreatic Cancer

Craig M. Goodwin et al.

Summary: Mutation of CDKN2A and activation of KRAS are crucial for the development and malignant growth of PDAC. Combination treatment with CDK4/6 and ERK-MAPK inhibitors synergistically suppresses the growth of PDAC cells and organoids by blocking compensatory upregulation of signaling pathways. CRISPR-Cas9 screening and protein activity mapping uncover novel combinations that enhance the potency of CDK4/6 inhibitors and overcome drug-induced compensations in PDAC.

CANCER RESEARCH (2023)

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Review Multidisciplinary Sciences

Recent medicinal approaches of novel pyrimidine analogs: A review

Sharanabasappa B. Patil

Summary: Pyrimidine derivatives have drawn the attention of researchers for their versatile structure and medicinal significance. Analogues associated with pyrimidine play a major role in medicinal chemistry. This review article highlights the recent advancements in the structural design and development of active agents, along with the biological approaches. It also discusses the structure-activity relationship and biological potency of various pyrimidines, including antimicrobial, anticancer, anti-inflammatory, analgesic, anti-diabetic, anti-HIV, anthelmintic, CNS depressants, and cardiac agents. Furthermore, this review article is expected to inspire researchers to design and develop novel active pyrimidine scaffolds that are more potent and less harmful.

HELIYON (2023)

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Review Chemistry, Medicinal

Heterocyclic pyrimidine derivatives as promising antibacterial agents

Kainat Ahmed et al.

Summary: Antibiotic resistance is a growing concern in public health, and understanding the mechanisms of drug resistance requires the development of new drugs. Pyrimidine compounds, due to their ease of functionalization, have become important in identifying new anti-bacterial agents. The presence of NH2 attached to the C-2 of the pyrimidine nucleus has been found to enhance the anti-bacterial activity against pathogenic bacteria. There is a need for a review on the synthesis and anti-bacterial activities of pyrimidine-containing compounds, considering the diversity of synthetic routes and the growing demand for novel anti-bacterial agents.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)

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Review Chemistry, Multidisciplinary

Advances in synthesis and biological activities of quinazoline scaffold analogues: A review

S. N. Murthy Boddapati et al.

Summary: This article discusses the synthesis protocols for quinazolines and their derivatives, highlighting the significant therapeutic activities of quinazoline-based drugs. It provides useful information for researchers to design and synthesize novel quinazoline analogues.

ARABIAN JOURNAL OF CHEMISTRY (2023)

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Review Chemistry, Multidisciplinary

An Updated Overview on the Synthesis and Anticancer Evaluation of Quinazoline Derivatives

Jasneet Kaur et al.

Summary: This comprehensive review outlines recent developments in the utilization of quinazoline derivatives as anticancer agents and offers insights into their potential as future anticancer drugs. By studying the structure-activity relationship, the review equips researchers with the necessary understanding for designing impactful quinazoline compounds with great potential in treating life-threatening disorders.

CHEMISTRYSELECT (2023)

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Review Oncology

RET Fusion-Positive Non-small Cell Lung Cancer: The Evolving Treatment Landscape

Silvia Novello et al.

Summary: This review provides a summary of available therapies for RET fusion-positive NSCLC, evaluating their efficacy and safety as well as primary and secondary resistance mechanisms. RET-selective inhibitors are recommended as first-line therapy options for these patients.

ONCOLOGIST (2023)

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Review Chemistry, Organic

A COMPREHENSIVE STUDY OF PYRIMIDINE AND ITS MEDICINAL APPLICATIONS

Vikas Vilas Borge et al.

Summary: Pyrimidine is a versatile compound that can be used as a lead compound for designing potent therapeutic agents. Different pyrimidine derivatives have various biological activities, including anticancer and antimicrobial effects. Studying the synthesis of pyrimidine and its derivatives is of great importance for understanding their pharmacological actions.

HETEROCYCLES (2022)

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Review Oncology

Mechanisms regulating PD-L1 expression in cancers and associated opportunities for novel small-molecule therapeutics

Hirohito Yamaguchi et al.

Summary: Antibodies targeting PD-1 or its ligand PD-L1 have greatly impacted cancer therapy by improving patient survival. Strategies to overcome resistance and understanding the underlying mechanisms of PD-L1 upregulation in malignancies are important. Small-molecule inhibitors show potential for targeting oncogenic pathways and modulating PD-L1 expression in cancer therapy.

NATURE REVIEWS CLINICAL ONCOLOGY (2022)

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Review Cell Biology

Re-Discovery of Pyrimidine Salvage as Target in Cancer Therapy

Melanie Walter et al.

Summary: Nucleotides can be synthesized through de novo synthesis and salvage pathways. Cancer cells can utilize the salvage pathway to maintain efficient DNA replication. However, the efficacy of pyrimidine de novo synthesis inhibitors in cancer treatment is limited. Therefore, targeting the pyrimidine salvage pathway in combination with other inhibitors has been suggested to overcome this limitation.

CELLS (2022)

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Review Oncology

A Therapeutic Journey of Pyridine-based Heterocyclic Compounds as Potent Anticancer Agents: A Review (From 2017 to 2021)

Munira Alrooqi et al.

Summary: Pyridine derivatives are common and significant heterocyclic compounds with diverse pharmacological properties. They exhibit potential therapeutic properties in various fields such as anti-bacterial, anti-viral, and anti-cancer, and are used to synthesize novel chemotherapeutic agents.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2022)

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Review Oncology

Heterocyclic Compounds: Importance in Anticancer Drug Discovery

Naresh Kumar et al.

Summary: Cancer is a crucial global health issue, being the second leading cause of global deaths, and with a rising trend in the number of cases in India. Researchers are focusing on developing novel anti-cancer drugs, with heterocyclic compounds showing promising pharmaceutical properties and being used in the discovery of new lead molecules.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2022)

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Article Oncology

Poor response to selpercatinib plus crizotinib in a rearranged during transfection fusion-positive patient with acquired selpercatinib-resistant MNNG HOS transforming amplification: a case report

Zhaoting Meng et al.

Summary: This study reported a case of lung adenocarcinoma initially treated with selpercatinib, which later developed resistance and switched to a combination of selpercatinib and crizotinib. However, the patient's condition rapidly deteriorated and she passed away after 4 months. The study emphasizes the need for future cohort studies to evaluate the efficacy of combining RET and MET inhibitors in treating RET-rearranged, MET-amplified NSCLC.

ANTI-CANCER DRUGS (2022)

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Article Chemistry, Medicinal

Topoisomerase I inhibitors: Challenges, progress and the road ahead

Arindam Talukdar et al.

Summary: Modulating the activity of Top1 in tumor cells has been identified as an important drug target for anticancer therapy. FDA-approved CPT derivatives have limitations, leading to interest in developing non-CPT Top1 poisons. This review provides a chronological development of different classes of Top1 poisons and discusses their application in combination therapies.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Pharmacology & Pharmacy

Tucatinib: an investigational novel therapeutic agent for the treatment of HER-2 colorectal cancer

Daniel Ahn et al.

Summary: HER-2 plays an important role in different types of cancers, including gastroesophageal, breast, and colorectal cancer. Tucatinib, as a selective HER-2 inhibitor, has shown potential therapeutic effects in a clinical setting. Although its role as a biomarker for prognosis in colorectal cancer remains uncertain, it is still a potential therapeutic target.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2022)

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Review Chemistry, Medicinal

Pyridine Moiety: An Insight into Recent Advances in the Treatment of Cancer

Rakesh Sahu et al.

Summary: This review discusses the importance of pyridine in the development of anticancer drugs, as well as its molecular docking, structure-activity relationship, market availability, and recent research works. Pyridine derivatives have wide applications in controlling and curing cancer, and researchers are currently focusing on the development of new pyridine-based drugs.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Recent research progress and outlook in agricultural chemical discovery based on quinazoline scaffold

Jixiang Chen et al.

Summary: The discovery of new scaffolds and targets for pesticides is a major challenge for sustainable agricultural development. Quinazoline derivatives have made significant progress in drug discovery and attracted great attention. Quinazoline, as a unique bicyclic scaffold, offers possibilities and flexibility for structural modification, making it an appealing candidate for discovering new pesticides. This article systematically reviews the agricultural biological activities, structure-activity relationships (SAR), and mechanism of action of quinazoline derivatives in the past decade, with a focus on SAR and mechanism. The authors also provide insights into the application of quinazoline scaffold in agricultural chemical discovery, aiming to inspire the rational design and mechanism of novel quinazoline agricultural chemicals in the future.

PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY (2022)

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Article Medicine, Research & Experimental

Operational complexity versus design efficiency: challenges of implementing a phase Ila multiple parallel cohort targeted treatment platform trial in advanced breast cancer

Claire Snowdon et al.

Summary: Platform trial designs are increasingly used in oncology clinical research and allow efficient evaluation of multiple targeted therapies. However, operational challenges can be overcome through multidisciplinary engagement, streamlined contracting processes, rationalized protocol and database design, and appropriate resourcing.

TRIALS (2022)

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Article Multidisciplinary Sciences

The evolution of RET inhibitor resistance in RET-driven lung and thyroid cancers

Ezra Y. Rosen et al.

Summary: The study has established the efficacy of the highly selective RET inhibitor selpercatinib in patients with RET-driven cancers, but also discovered potential mechanisms of resistance, revealing the complexity of acquired resistance and suggesting the importance of combination therapy targeting alternative pathways in overcoming resistance.

NATURE COMMUNICATIONS (2022)

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Review Chemistry, Multidisciplinary

A review on synthetic investigation for quinoline- recent green approaches

Ashish Patel et al.

Summary: Quinolines are important heterocyclic motifs and are crucial for creating physiologically active compounds. Traditional synthesis methods often require expensive and demanding conditions, resulting in environmental harm. Scientists are currently developing new green synthesis methods to reduce the use of harmful chemicals.

GREEN CHEMISTRY LETTERS AND REVIEWS (2022)

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Review Chemistry, Multidisciplinary

Recent Advances in Synthesis of Multiply Arylated/Alkylated Pyridines

Annisa Indah Reza et al.

Summary: This review discusses recent advances in the synthesis of aryl/alkyl-substituted pyridines, grouping reaction patterns that generally produce tri-, tetra-, and penta-aryl/alkyl pyridines.

CHEMICAL RECORD (2022)

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Review Biochemistry & Molecular Biology

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

Oluwakemi Ebenezer et al.

Summary: Heterocyclic compounds are natural compounds with favorable properties and significant pharmaceutical importance. They have diverse applications as smart biomimetics and possess active pharmacophores in complex structures, making them indispensable in drug discovery. Among different heterocyclic ring systems, nitrogen heterocyclic compounds are more abundant in nature and have considerable pharmacological significance. This review highlights pioneering studies in the biological assessment of nitrogen-containing compounds, such as triazoles, tetrazoles, imidazole/benzimidazoles, pyrimidines, and quinolines. It covers publications from April 2020 to February 2022 and will be beneficial for researchers in medicinal chemistry and pharmacology.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

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Review Chemistry, Multidisciplinary

A Mini Review on the Multicomponent Synthesis of Pyridine Derivatives

S. Lokesh Kumar et al.

Summary: The article briefly reviews the literature on the synthesis of substituted pyridine using multicomponent approaches from 2016 to early 2022. Multicomponent reactions have emerged as a key green tool in organic synthesis, playing a crucial role in the diversification of heterocycle synthesis.

CHEMISTRYSELECT (2022)

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Article Biochemistry & Molecular Biology

Ceritinib is a novel triple negative breast cancer therapeutic agent

Shengli Dong et al.

Summary: Combination therapy with ceritinib and enzalutamide inhibits the growth of AR(+) TNBC cells, while combination therapy with ceritinib and paclitaxel drastically inhibits tumor growth. These findings suggest that combination treatment with these FDA-approved drugs can improve the therapeutic response in both AR-positive and negative breast cancer.

MOLECULAR CANCER (2022)

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Review Chemistry, Multidisciplinary

Review on recent development of quinoline for anticancer activities

Mohan Ilakiyalakshmi et al.

Summary: This article summarizes the effectiveness of quinoline and its derivatives as efficient scaffolds for anticancer drug development, demonstrating their potent anticancer potential through mechanisms such as apoptosis, disruption of cell migration, inhibition of angiogenesis, modulation of nuclear receptor responsiveness, and cell cycle arrest.

ARABIAN JOURNAL OF CHEMISTRY (2022)

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Review Chemistry, Multidisciplinary

Environmentally Benign Approaches towards the Synthesis of Quinolines

Asim Kumar et al.

Summary: This article reviews notable synthetic methodologies of quinoline in the past decade, with a focus on achieving sustainability in synthesis. The review highlights sustainable and environmentally friendly approaches such as solvent-free reactions, the use of alternate reaction media, and alternative modes of synthesis like microwave-assisted synthesis and flow reactions.

CHEMISTRYSELECT (2022)

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Review Oncology

Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021

Qing Wu et al.

Summary: The US FDA has been at the forefront of drug evaluation and supervision. Over the past 31 years, 1050 drugs have been approved, with 228 of them being cancer therapeutics or cancer-related drugs. These drugs have evolved from broad-spectrum antitumor small molecules to more precise monoclonal antibodies and antibody-drug conjugates. However, the development of antitumor drugs is still limited by the available targets, mainly receptor tyrosine kinases.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2022)

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Article Chemistry, Multidisciplinary

Unified Access to Pyrimidines and Quinazolines Enabled by N-N Cleaving Carbon Atom Insertion

Ethan E. Hyland et al.

Summary: Given the prevalence of heterocycles in biologically active compounds, it is highly desirable to develop reactions that can modify such molecular skeletons with modularity. Ring expansion reactions that enable interconversion of different heterocyclic motifs are particularly interesting. In this study, we report a reaction that selectively cleaves the N-N bond of pyrazole and indazole cores to produce pyrimidines and quinazolines, respectively. This reaction mediated by chlorodiazirine provides a unified route to a related pair of heterocycles that are typically prepared using different methods.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2022)

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Review Chemistry, Organic

Chemistry of Quinolines and their Agrochemical Potential

Divya Utreja et al.

Summary: The increasing human population puts pressure on agriculture and food supply, while crop production is hindered by pathogenic infections. Quinoline, a nitrogen-containing heterocyclic compound, has drawn attention for its diverse chemical and biological activities. This review focuses on the synthesis and agrochemical potential of various quinoline derivatives.

CURRENT ORGANIC CHEMISTRY (2022)

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Review Chemistry, Multidisciplinary

Pyridine: the scaffolds with significant clinical diversity

Sourav De et al.

Summary: This article summarizes the latest advances in novel pyridine-based molecular frameworks and their clinical relevance over the past two decades. It highlights the trend of using pyridine-based molecules in drug design and the emergence of several effective drug candidates against various diseases.

RSC ADVANCES (2022)

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Review Oncology

Bestowal of Quinazoline Scaffold in Anticancer Drug Discovery

Rina Das et al.

Summary: Quinazoline derivatives have emerged as a promising class of anticancer agents, with studies showing significant anticancer activity through multiple mechanisms. Future exploration of the potential of these derivatives is needed to enhance chemotherapy efficacy in cancer treatment.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2021)

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Review Chemistry, Medicinal

Quinoline-based Compounds with Potential Activity against Drug-resistant Cancers

Huan-Ting Li et al.

Summary: Drug resistance is a major cause of cancer chemotherapy failure, and overcoming drug resistance is essential in developing effective cancer therapeutic strategies. Quinoline-based compounds such as Anlotinib have been used in clinical practice to fight against cancers, showing potential as anticancer agents.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2021)

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Article Oncology

Phase III, Randomized Study of Dual Human Epidermal Growth Factor Receptor 2 (HER2) Blockade With Lapatinib Plus Trastuzumab in Combination With an Aromatase Inhibitor in Postmenopausal Women With HER2-Positive, Hormone Receptor-Positive Metastatic Breast Cancer: Updated Results of ALTERNATIVE

Stephen R. D. Johnston et al.

Summary: Dual HER2 blockade with LAP plus TRAS plus AI showed superior progression-free survival (PFS) benefit versus TRAS plus AI in patients with HER2-positive/HR-positive MBC. This combination offers an effective and safe chemotherapy-sparing alternative treatment regimen for this patient population. Common adverse events were mostly grade 1 or 2 and serious adverse events were reported similarly across the three groups.

JOURNAL OF CLINICAL ONCOLOGY (2021)

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Review Chemistry, Organic

Recent synthetic methodologies for the tricyclic fused-quinoline derivatives

Furqan Ahmad Saddique et al.

Summary: Tricyclic fused-quinoline ring system is a fascinating and versatile class of heterocycles with a wide spectrum of biological activities. They can be synthesized through various efficient synthetic routes, including multicomponent reactions, transition metal catalysis, etc. This review focuses on the factors affecting product yields, selectivities, and the applications of these methods in obtaining valuable candidates in the past five years.

SYNTHETIC COMMUNICATIONS (2021)

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Review Chemistry, Medicinal

Recent update on antibacterial and antifungal activity of quinoline scaffolds

Atukuri Dorababu

Summary: Although most heterocycles have significant pharmacological activities, only a few quinoline derivatives exhibit the best biological activities, including anticancer, anti-inflammatory, antibacterial, antiviral, and antifungal activities. Therefore, designing more efficient antimicrobial drugs is a priority to prevent malevolent microbial diseases.

ARCHIV DER PHARMAZIE (2021)

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Review Biochemistry & Molecular Biology

Quinolines, a perpetual, multipurpose scaffold in medicinal chemistry

Pratibha Yadav et al.

Summary: Quinoline is a versatile pharmacophore with a wide range of pharmacological activities, and quinoline hybrids have shown promising anticancer, anti-inflammatory, antibacterial, and other activities. Numerous studies have summarized the recent advances of quinoline derivatives, helping in the development of clinically viable drug candidates for the treatment of incurable diseases.

BIOORGANIC CHEMISTRY (2021)

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Article Oncology

Comparative analysis of drug response and gene profiling of HER2-targeted tyrosine kinase inhibitors

Neil T. Conlon et al.

Summary: The study compared the anti-proliferative effects of three HER2-targeted drugs on cancer cell lines, showing neratinib to be the most effective against HER2-positive as well as HER2 and EGFR mutant cells. The research also identified novel biomarkers associated with drug response and resistance.

BRITISH JOURNAL OF CANCER (2021)

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Article Pharmacology & Pharmacy

Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma

Gehan Botrus et al.

Summary: The FGFR pathway plays a crucial role in cell functions, especially in cancers like IHCA. Infigratinib, as an FGFR inhibitor, has shown promising results in preclinical studies and is being investigated for cancer treatment. Ongoing phase III clinical trials are evaluating its efficacy in treating IHCA with FGFR2 fusions compared to standard treatments.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2021)

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Review Chemistry, Medicinal

Current Pharmaceutical Aspects of Synthetic Quinoline Derivatives

Rukhsana Tabassum et al.

Summary: Quinoline derivatives are widely used in the treatment of various diseases due to their broad spectrum of biological activities. The focus of research is on the anti-viral, anti-cancer, and anti-fungal properties of quinoline compounds.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2021)

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Article Oncology

Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations

V Subbiah et al.

Summary: The study revealed that RET mutations resistant to selpercatinib and pralsetinib mainly located at the solvent front and hinge regions in medullary thyroid cancer and non-small-cell lung cancer. The unconventional binding mode of selpercatinib and pralsetinib to RET avoids interference from gatekeeper mutations but is susceptible to non-gatekeeper mutations.

ANNALS OF ONCOLOGY (2021)

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Article Oncology

Abemaciclib in combination with endocrine therapy for East Asian patients with HR+, HER2-advanced breast cancer: MONARCH 2 & 3 trials

Masakazu Toi et al.

Summary: In East Asian patients with HR+, HER2- advanced breast cancer, abemaciclib in combination with ET demonstrated significantly prolonged progression-free survival, with generally tolerable safety profiles. Pharmacokinetics were similar between East Asians and non-East Asians in both MONARCH 2 and MONARCH 3 trials.

CANCER SCIENCE (2021)

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Article Chemistry, Medicinal

US FDA Approved Drugs from 2015-June 2020: A Perspective

Priyadeep Bhutani et al.

Summary: This study compiled and analyzed 245 drugs approved by the U.S. FDA from 2015 to June 2020, focusing on cancer, infectious diseases, neurological conditions, and genetic, metabolic, cardiovascular disorders. The analysis also looked at the structural, elemental, and functional group diversity among the approved drugs, as well as drug-likeness for the approved drugs.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Review Chemistry, Medicinal

Quinoline: An Attractive Scaffold in Drug Design

Lucas F. E. Moor et al.

Summary: Quinoline and its derivatives, important heterocyclic compounds, have shown a wide range of pharmacological properties such as anticancer, antiparasitic, and antimalarial activities in recent years.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2021)

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Review Pharmacology & Pharmacy

Encorafenib: A Review in Metastatic Colorectal Cancer with a BRAF V600E Mutation

Zaina T. Al-Salama

Summary: Encorafenib in combination with cetuximab has shown significantly longer overall survival, higher response rate, and better tolerability in patients with mCRC and a BRAF V600E mutation who have had prior therapy.

DRUGS (2021)

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Editorial Material Gastroenterology & Hepatology

Infigratinib in pretreated cholangiocarcinoma with FGFR2 fusions or rearrangements

Cindy Neuzillet

LANCET GASTROENTEROLOGY & HEPATOLOGY (2021)

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Review Oncology

Non-Small-Cell Lung Cancer: New Rare Targets-New Targeted Therapies-State of The Art and Future Directions

Katarzyna Stencel et al.

Summary: The use of novel therapeutic drugs in lung cancer has revolutionized the diagnosis and treatment paradigms, with many new targeted therapies approved by the FDA or in clinical trials. Lung cancer remains a leading cause of cancer-related deaths globally, and specific genetic alterations indicate the suitability for targeted therapies.

CANCERS (2021)

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Article Pharmacology & Pharmacy

Real-Time Positron Emission Tomography Evaluation of Topotecan Brain Kinetics after Ultrasound-Mediated Blood-Brain Barrier Permeability

Andrei Molotkov et al.

Summary: Glioblastoma is a common primary brain malignancy with poor prognosis, largely due to the blood-brain barrier restricting therapeutic delivery. High-intensity focused ultrasound with microbubbles can potentially improve drug penetration into the brain.

PHARMACEUTICS (2021)

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Review Oncology

Clinical pharmacology and drug-drug interactions of lenvatinib in thyroid cancer

Stefano Fogli et al.

Summary: Lenvatinib is a non-selective tyrosine kinase inhibitor that is most effective in patients with thyroid cancer. The drug is well tolerated and common adverse reactions can be managed by dose adjustment. Monitoring of blood pressure and cardiac function may be required during treatment.

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2021)

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Review Chemistry, Organic

Synthetic Aspects of Condensed Pyrimidine Derivatives

Meenu Devi et al.

Summary: This review focuses on the synthesis of pyrimidine derivatives with various activities, encouraging researchers to develop novel, potent, safe, and selective compounds against mutant strains. Development of synthetic protocols is a high priority in medicinal chemistry research.

CURRENT ORGANIC CHEMISTRY (2021)

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Review Chemistry, Organic

Synthetic and Biological Attributes of Pyrimidine Derivatives: A Recent Update

Meenu Devi et al.

Summary: Nitrogen-containing heterocycles, particularly pyrimidine, have drawn significant attention from chemists due to their diverse biological activities and potential therapeutic applications. Pyrimidine derivatives, with their high degree of structural diversity, exhibit a wide range of therapeutic activities such as anticancer, anti-inflammatory, and anti-HIV properties.

CURRENT ORGANIC SYNTHESIS (2021)

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Review Chemistry, Medicinal

Current Status of Novel Pyridine Fused Derivatives as Anticancer Agents: An Insight into Future Perspectives and Structure Activity Relationship (SAR)

Ajay Manaithiya et al.

Summary: Cancer, a prevalent heterogeneous disease, calls for more effective drugs. Oxygen and nitrogen-based heterocyclic compounds have shown therapeutic activity, with pyrido fused five-membered heterocyclic rings being highlighted as important anticancer drugs.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Recent contributions of quinolines to antimalarial and anticancer drug discovery research

Tim Van de Walle et al.

Summary: Quinoline, a privileged scaffold in medicinal chemistry, plays a central role in antimalarial and anticancer research, but established quinoline-containing antimalarial drugs are facing widespread resistance. On the other hand, there is a growing interest in quinoline compounds as potential anticancer agents.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Review Oncology

RET Inhibitors in Non-Small-Cell Lung Cancer

Priscilla Cascetta et al.

Summary: RET rearrangements in NSCLC act as a potential therapeutic target, with selective RET inhibitors showing higher efficacy rates and good tolerability, providing hope for patients with RET-positive NSCLC. Ongoing phase III clinical trials will definitively establish the efficacy of these inhibitors in RET-positive NSCLC patients.

CANCERS (2021)

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Review Oncology

HER2-positive breast cancer and tyrosine kinase inhibitors: the time is now

Ilana Schlam et al.

Summary: HER2-positive breast cancer accounts for a significant proportion of cases, with several targeted therapies available including TKIs which have shown promising responses in both early and advanced settings. In patients with central nervous system involvement, TKIs have shown efficacy, which is important for those with limited treatment options and poor prognosis in this setting.

NPJ BREAST CANCER (2021)

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Review Pharmacology & Pharmacy

Recent Development in Nuclear Magnetic Resonance as a Technique for Quantitative Method Validation

R. Sahu et al.

Summary: Nuclear magnetic resonance spectroscopy has been widely used for the routine analysis of natural, synthetic drug candidates, and related molecules. This review focuses on the feasibility and effectiveness of using nuclear magnetic resonance for quantitative method validation of drugs and related compounds, showing that it is a reliable alternative to chromatography-based techniques for quantitative analysis.

INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES (2021)

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Review Chemistry, Multidisciplinary

Recent developments in the synthesis of polysubstituted pyridines via multicomponent reactions using nanocatalysts

Fatemeh Majidi Arlan et al.

Summary: This review focuses on the application of various types of nanoparticles as catalysts in the synthesis of pyridine derivatives via multicomponent reactions in the past decade (2010-2020), demonstrating the creation of novel active pharmacophores by chemists.

NEW JOURNAL OF CHEMISTRY (2021)

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Article Oncology

Expression of the Body-Weight Signaling Players: GDF15, GFRAL and RET and their clinical relevance in Gastric Cancer

Karolina Buchholz et al.

Summary: The protein expression of GDF15, GFRAL, and RET is significantly elevated and positively correlated in GC tissues, showing a tendency to be overexpressed in low and intermediate-grade tumors. High GDF15 expression is associated with better overall survival, while high levels of GFRAL and RET are associated with poor overall survival. The combined expression of GDF15, GFRAL, and RET is significantly associated with reduced overall survival and is an independent prognostic factor with borderline significance.

JOURNAL OF CANCER (2021)

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Review Chemistry, Organic

Visible-light-mediated synthesis of quinolines

Ajay Kumar Dhiya et al.

Summary: Quinolines are widely used in various fields, but traditional synthesis methods have drawbacks, prompting the shift towards light-catalyzed synthesis. This review focuses on recent research on the synthesis of quinolines using visible light.

ORGANIC CHEMISTRY FRONTIERS (2021)

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Review Chemistry, Multidisciplinary

Research developments in the syntheses, anti-inflammatory activities and structure-activity relationships of pyrimidines

Haroon Ur Rashid et al.

Summary: Pyrimidines are aromatic heterocyclic compounds with diverse pharmacological effects, including anti-inflammatory properties. This review highlights recent developments in the synthesis, anti-inflammatory effects, and structure-activity relationships of pyrimidine derivatives, suggesting potential research directions for developing new pyrimidines with enhanced anti-inflammatory activities.

RSC ADVANCES (2021)

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Review Chemistry, Multidisciplinary

The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

Oleksandr O. Grygorenko et al.

CHEMISTRY-A EUROPEAN JOURNAL (2020)

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Review Chemistry, Multidisciplinary

Organocatalyzed Synthesis of Functionalized Quinolines

Lian-Hua Li et al.

CHEMISTRY-AN ASIAN JOURNAL (2020)

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Article Chemistry, Organic

Three Step Synthesis of Fully and Differently Arylated Pyridines

Mao Arita et al.

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY (2020)

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Article Oncology

RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies

Benjamin J. Solomon et al.

JOURNAL OF THORACIC ONCOLOGY (2020)

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Review Oncology

Somatic Mutations in HER2 and Implications for Current Treatment Paradigms in HER2-Positive Breast Cancer

Maria Gaibar et al.

JOURNAL OF ONCOLOGY (2020)

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Review Chemistry, Organic

Recent Progress in the Synthesis of Pyrimidine Heterocycles: A Review

Pradip Kumar Maji

CURRENT ORGANIC CHEMISTRY (2020)

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Review Biochemistry & Molecular Biology

CDKs in Sarcoma: Mediators of Disease and Emerging Therapeutic Targets

Jordan L. Kohlmeyer et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

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Review Oncology

Medical oncology management of advanced hepatocellular carcinoma 2019: a reality check

Amy Lee et al.

FRONTIERS OF MEDICINE (2020)

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Article Chemistry, Organic

NH4I-Triggered [4+2] Annulation of α,β-Unsaturated Ketoxime Acetates with N-Acetyl Enamides for the Synthesis of Pyridines

Jindian Duan et al.

JOURNAL OF ORGANIC CHEMISTRY (2020)

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Article Oncology

Imaging Features and Patterns of Metastasis in Non-Small Cell Lung Cancer with RET Rearrangements

Subba R. Digumarthy et al.

CANCERS (2020)

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Review Oncology

Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview

Damanpreet K. Lang et al.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2020)

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Review Chemistry, Organic

Recent Advances in Transition Metal Free Synthetic Protocols for Quinoline Derivatives

Rukhsana Tabassum et al.

CURRENT ORGANIC CHEMISTRY (2020)

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Article Pharmacology & Pharmacy

Tucatinib: First Approval

Arnold Lee

DRUGS (2020)

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Article Oncology

Neratinib in patients with HER2-mutant, metastatic cervical cancer: Findings from the phase 2 SUMMIT basket trial

Ana Oaknin et al.

GYNECOLOGIC ONCOLOGY (2020)

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Article Integrative & Complementary Medicine

RalB degradation by dihydroartemisinin induces autophagy and IFI16/caspase-1 inflammasome depression in the human laryngeal squamous cell carcinoma

Xinli Shi et al.

CHINESE MEDICINE (2020)

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Review Chemistry, Physical

Quinoline and its derivatives as corrosion inhibitors: A review

Chandrabhan Verma et al.

SURFACES AND INTERFACES (2020)

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Review Chemistry, Medicinal

Recent Development of Pyrimidine-Containing Antimicrobial Agents

Jianxing Zhuang et al.

CHEMMEDCHEM (2020)

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Review Chemistry, Multidisciplinary

Prescribed drugs containing nitrogen heterocycles: an overview

Majid M. Heravi et al.

RSC ADVANCES (2020)

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Article Oncology

Systemic and CNS Activity of Selective RET Inhibition With Selpercatinib (LOXO-292) in a Patient With RET-Mutant Medullary Thyroid Cancer With Extensive CNS Metastases

Alexander Andreev-Drakhlin et al.

JCO PRECISION ONCOLOGY (2020)

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Review Pharmacology & Pharmacy

Dacomitinib in the Management of Advanced Non-Small-Cell Lung Cancer

Sally C. M. Lau et al.

DRUGS (2019)

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Article Chemistry, Organic

Synthesis of Quinazoline and Quinazolinone Derivatives via Ligand-Promoted Ruthenium-Catalyzed Dehydrogenative and Deaminative Coupling Reaction of 2-Aminophenyl Ketones and 2-Aminobenzamides with Amines

Pandula T. Kirinde Arachchige et al.

ORGANIC LETTERS (2019)

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Article Oncology

Prognostic implications of a molecular classifier derived from whole-exome sequencing in nasopharyngeal carcinoma

Hai-Yun Wang et al.

CANCER MEDICINE (2019)

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Review Oncology

Lenvatinib, a molecule with versatile application: from preclinical evidence to future development in anti-cancer treatment

Monica Capozzi et al.

CANCER MANAGEMENT AND RESEARCH (2019)

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Review Oncology

Diverse Mechanisms of BRAF Inhibitor Resistance in Melanoma Identified in Clinical and Preclinical Studies

Stephen A. Luebker et al.

FRONTIERS IN ONCOLOGY (2019)

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Review Chemistry, Organic

Recent Progress in the Synthesis of Quinolines

Duc Dau Xuan

CURRENT ORGANIC SYNTHESIS (2019)

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Article Chemistry, Organic

DBU-Mediated Cyclization of Acylcyclopropanecarboxylates with Amidines: Access to Polysubstituted Pyrimidines

Shan Wang et al.

ORGANIC LETTERS (2019)

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Article Chemistry, Organic

Heterogeneous gold(I)-catalyzed cyclization between ynals and amidines: An efficient and practical synthesis of 2,4-disubstituted pyrimidines

Minhua Jiang et al.

SYNTHETIC COMMUNICATIONS (2019)

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Review Oncology

NF-κB/Rel Transcription Factors in Pancreatic Cancer: Focusing on RelA, c-Rel, and RelB

Derya Kabacaoglu et al.

CANCERS (2019)

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Article Cell Biology

MDM2 antagonists overcome intrinsic resistance to CDK4/6 inhibition by inducing p21

Anna E. Vilgelm et al.

SCIENCE TRANSLATIONAL MEDICINE (2019)

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Article Chemistry, Multidisciplinary

Development of a Split Esterase for Protein-Protein Interaction-Dependent Small-Molecule Activation

Krysten A. Jones et al.

ACS CENTRAL SCIENCE (2019)

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Review Oncology

The PI3K/AKT/mTOR and CDK4/6 Pathways in Endocrine Resistant HR+/HER2-Metastatic Breast Cancer: Biological Mechanisms and New Treatments

Daniele Presti et al.

CANCERS (2019)

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Review Oncology

RET fusions in solid tumors

Andrew Y. Li et al.

CANCER TREATMENT REVIEWS (2019)

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Article Gastroenterology & Hepatology

Infigratinib Mediates Vascular Normalization, Impairs Metastasis, and Improves Chemotherapy in Hepatocellular Carcinoma

Hung Huynh et al.

HEPATOLOGY (2019)

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Article Chemistry, Medicinal

A Survey of the Structures of US FDA Approved Combination Drugs

Pradipta Das et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

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Review Chemistry, Medicinal

Topoisomerase 1B poisons: Over a half-century of drug leads, clinical candidates, and serendipitous discoveries

Maris A. Cinelli

MEDICINAL RESEARCH REVIEWS (2019)

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Article Parasitology

Topoisomerase IB poisons induce histone H2A phosphorylation as a response to DNA damage in Leishmania infantum

Camino Gutierrez-Corbo et al.

INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE (2019)

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Article

Quinazoline compounds for antitumor treatment

G.I. Solyanik

Experimental Oncology (2019)

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Review Cell Biology

The therapeutic potential of targeting the BRAF mutation in patients with colorectal cancer

Afsane Bahrami et al.

JOURNAL OF CELLULAR PHYSIOLOGY (2018)

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Article Pharmacology & Pharmacy

Drug resistance profiles of mutations in the RET kinase domain

Xuan Liu et al.

BRITISH JOURNAL OF PHARMACOLOGY (2018)

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Review Oncology

Management of QT prolongation induced by anti-cancer drugs: Target therapy and old agents. Different algorithms for different drugs

Carmela Coppola et al.

CANCER TREATMENT REVIEWS (2018)

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Review Oncology

Systemic therapy for intermediate and advanced hepatocellular carcinoma: Sorafenib and beyond

Jean-Luc Raoul et al.

CANCER TREATMENT REVIEWS (2018)

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Article Oncology

US Food and Drug Administration Approval: Neratinib for the Extended Adjuvant Treatment of Early-Stage HER2-Positive Breast Cancer

Harpreet Singh et al.

CLINICAL CANCER RESEARCH (2018)

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Article Chemistry, Organic

Palladium-Catalyzed Aerobic Oxidative Coupling of Allylic Alcohols with Anilines in the Synthesis of Nitrogen Heterocycles

Gangam Srikanth Kumar et al.

JOURNAL OF ORGANIC CHEMISTRY (2018)

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Article Chemistry, Organic

Copper-Catalyzed Synthesis of Substituted Quinazolines from Benzonitriles and 2-Ethynylanilines via Carbon-Carbon Bond Cleavage Using Molecular Oxygen

Xu Wang et al.

JOURNAL OF ORGANIC CHEMISTRY (2018)

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Article Chemistry, Organic

Straightforward synthesis of quinolines from enones and 2-aminobenzyl alcohols using an iridium-catalyzed transfer hydrogenative strategy

Biao Xiong et al.

ORGANIC & BIOMOLECULAR CHEMISTRY (2018)

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Article Chemistry, Multidisciplinary

Reactivity of highly Lewis acidic diborane(4) towards pyridine and isocyanide: formation of boraalkene-pyridine complex and ortho-functionalized pyridine derivatives

Yuhei Katsuma et al.

CHEMICAL SCIENCE (2018)

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Article Chemistry, Organic

Palladium-Catalyzed Regioselective Cyclocarbonylation of N-(3-Phenylprop-2-ynyl)anilines with Carbon Monoxide and Alcohols for the Synthesis of Quinoline-3-carboxylic Esters

Wei Zhang et al.

ASIAN JOURNAL OF ORGANIC CHEMISTRY (2018)

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Article Chemistry, Organic

Base-Promoted Synthesis of 2,4,6-Triarylpyridines from Enaminones and Chalcones

Hong Zhang et al.

ASIAN JOURNAL OF ORGANIC CHEMISTRY (2018)

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Article Chemistry, Organic

Photoredox-catalyzed cascade addition/cyclization of N-propargyl aromatic amines: access to 3-difluoroacetylated or 3-fluoroacetylated quinolines

Qinfei Deng et al.

ORGANIC CHEMISTRY FRONTIERS (2018)

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Article Chemistry, Applied

Gold-Catalyzed Intermolecular [4+2] Annulation of 2-Ethynylanilines with Ynamides: An Access to Substituted 2-Aminoquinolines

Ximei Zhao et al.

ADVANCED SYNTHESIS & CATALYSIS (2018)

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Article Pharmacology & Pharmacy

Dacomitinib: First Global Approval

Matt Shirley

DRUGS (2018)

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Review Pharmacology & Pharmacy

Afatinib and Erlotinib in the treatment of squamous-cell lung cancer

Marco Tagliamento et al.

EXPERT OPINION ON PHARMACOTHERAPY (2018)

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Article Chemistry, Organic

N-Silylenamines as Reactive Intermediates: Hydroamination for the Modular Synthesis of Selectively Substituted Pyridines

Erica K. J. Lui et al.

ORGANIC LETTERS (2018)

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Review Oncology

Drug review: Pazopanib

Shingo Miyamoto et al.

JAPANESE JOURNAL OF CLINICAL ONCOLOGY (2018)

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Article Health Care Sciences & Services

Cost-effectiveness analysis of ribociclib versus palbociclib in the first-line treatment of HR+/HER2- advanced or metastatic breast cancer in Spain

Elena Galve-Calvo et al.

CLINICOECONOMICS AND OUTCOMES RESEARCH (2018)

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Article Allergy

Increase of poorly proliferated p63+/Ki67+ basal cells forming multiple layers in the aberrant remodeled epithelium in nasal polyps

L. Zhao et al.

ALLERGY (2017)

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Letter Oncology

Gefitinib or Erlotinib for Previously Treated Lung Adenocarcinoma: Which Is Superior?

Chia-Hao Chang et al.

JOURNAL OF CLINICAL ONCOLOGY (2017)

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Article Chemistry, Organic

Iron Catalysis for Modular Pyrimidine Synthesis through β-Ammoniation/Cyclization of Saturated Carbonyl Compounds with Amidines

Xue-Qiang Chu et al.

JOURNAL OF ORGANIC CHEMISTRY (2017)

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Review Oncology

Targeted agents and immunotherapies: optimizing outcomes in melanoma

Jason J. Luke et al.

NATURE REVIEWS CLINICAL ONCOLOGY (2017)

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Article Chemistry, Organic

Traceless Directing-Group Strategy in the Ru-Catalyzed, Formal [3+3] Annulation of Anilines with Allyl Alcohols: A One-Pot, Domino Approach for the Synthesis of Quinolines

Gangam Srikanth Kumar et al.

ORGANIC LETTERS (2017)

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Article Endocrinology & Metabolism

Distribution of RET Mutations in Multiple Endocrine Neoplasia 2 in Denmark 1994-2014: A Nationwide Study

Jes Sloth Mathiesen et al.

THYROID (2017)

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Article Multidisciplinary Sciences

CDK4/6 and autophagy inhibitors synergistically induce senescence in Rb positive cytoplasmic cyclin E negative cancers

Smruthi Vijayaraghavan et al.

NATURE COMMUNICATIONS (2017)

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Article Chemistry, Organic

Cu-Catalyzed intermolecular [3+3] annulation involving oxidative activation of an unreactive C(sp3)-H bond: access to pyrimidine derivatives from amidines and ketones

Wei Guo et al.

ORGANIC CHEMISTRY FRONTIERS (2017)

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Article Genetics & Heredity

Downregulation of miR-503 Promotes ESCC Cell Proliferation, Migration, and Invasion by Targeting Cyclin D1

Lanfang Jiang et al.

GENOMICS PROTEOMICS & BIOINFORMATICS (2017)

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Article Multidisciplinary Sciences

Effects of RET, NRG1 and NRG3 Polymorphisms in a Chinese Population with Hirschsprung Disease

Dehua Yang et al.

SCIENTIFIC REPORTS (2017)

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Review Oncology

Escalating and de-escalating treatment in HER2-positive early breast cancer

Heikki Joensuu

CANCER TREATMENT REVIEWS (2017)

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Review Medicine, Research & Experimental

The role of pazopanib on tumour angiogenesis and in the management of cancers: A review

Dinesh Kumar Chellappan et al.

BIOMEDICINE & PHARMACOTHERAPY (2017)

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Review Oncology

Systemic treatment of renal cell cancer: A comprehensive review

Amparo Sanchez-Gastaldo et al.

CANCER TREATMENT REVIEWS (2017)

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Article Chemistry, Applied

Lewis Acid-Mediated [3+3] Annulation for the Construction of Substituted Pyrimidine and Pyridine Derivatives

Yao Zhou et al.

ADVANCED SYNTHESIS & CATALYSIS (2017)

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Article Chemistry, Multidisciplinary

Tailor-made synthesis of fully alkylated/arylated nicotinates by FeCl3-mediated condensation of enamino esters with enones

Sho Hirai et al.

CHEMICAL COMMUNICATIONS (2017)

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Article Chemistry, Applied

An Unexpected Construction of 2-Arylquinolines from N-Cinnamylanilines through sp3 C-H Aerobic Oxidation Induced by a Catalytic Radical Cation Salt

Fang Liu et al.

ADVANCED SYNTHESIS & CATALYSIS (2016)

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Article Oncology

NTRK fusion oncogenes in pediatric papillary thyroid carcinoma in northeast United States

Manju L. Prasad et al.

CANCER (2016)

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Article Chemistry, Organic

Transition Metal Free Intermolecular Direct Oxidative C-N Bond Formation to Polysubstituted Pyrimidines Using Molecular Oxygen as the Sole Oxidant

Wei Guo et al.

JOURNAL OF ORGANIC CHEMISTRY (2016)

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Article Chemistry, Organic

Palladium-Catalyzed Allylic C-H Oxidative Annulation for Assembly of Functionalized 2-Substituted Quinoline Derivatives

Chunsheng Li et al.

JOURNAL OF ORGANIC CHEMISTRY (2016)

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Article Chemistry, Organic

Visible-Light-Induced Photocatalytic Aerobic Oxidation/Povarov Cyclization Reaction: Synthesis of Substituted Quinoline-Fused Lactones

Wuheng Dong et al.

JOURNAL OF ORGANIC CHEMISTRY (2016)

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Article Oncology

A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger et al.

MOLECULAR CANCER THERAPEUTICS (2016)

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Review Biochemistry & Molecular Biology

Recent Advances in Metal-Free Quinoline Synthesis

Ginelle A. Ramann et al.

MOLECULES (2016)

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Article Chemistry, Organic

An economical synthesis of substituted quinoline-2-carboxylates through the potassium persulfate-mediated cross-dehydrogenative coupling of N-aryl glycine derivatives with olefins

Guoliang Liu et al.

ORGANIC & BIOMOLECULAR CHEMISTRY (2016)

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Article Chemistry, Organic

tert-Butyl Hydroperoxide Mediated Cascade Synthesis of 3-Arylsulfonylquinolines

Liangliang Zhang et al.

ORGANIC LETTERS (2016)

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Article Chemistry, Organic

Rh- and Cu-Cocatalyzed Aerobic Oxidative Approach to Quinazolines via [4+2] C-H Annulation with Alkyl Azides

Xiaoyang Wang et al.

ORGANIC LETTERS (2016)

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Review Oncology

Ceritinib: a Review in ALK-Positive Advanced NSCLC

Emma D. Deeks

TARGETED ONCOLOGY (2016)

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Review Biotechnology & Applied Microbiology

Dabrafenib: a new opportunity for the treatment of BRAF V600-positive melanoma

Maria Banzi et al.

ONCOTARGETS AND THERAPY (2016)

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Article Chemistry, Organic

Cobalt-catalyzed synthesis of quinolines from the redox-neutral annulation of anilides and alkynes

Qiangqiang Yan et al.

ORGANIC CHEMISTRY FRONTIERS (2016)

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Review Oncology

Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib

Vera Hirsh

BIODRUGS (2015)

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Article Endocrinology & Metabolism

Early and Late G1/S Cyclins and Cdks Act Complementarily to Enhance Authentic Human β-Cell Proliferation and Expansion

Shiwani Tiwari et al.

DIABETES (2015)

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Article Chemistry, Medicinal

Design, synthesis and evaluation of thiohydantoin derivatives as potent topoisomerase I (Top1) inhibitors with anticancer activity

Papiya Majumdar et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)

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Article Biochemistry & Molecular Biology

A Comprehensive Transcriptomic and Proteomic Analysis of Hydra Head Regeneration

Hendrik O. Petersen et al.

MOLECULAR BIOLOGY AND EVOLUTION (2015)

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Article Chemistry, Organic

Modular Synthesis of Highly Substituted Pyridines via Enolate α-Alkenylation

Leo A. Hardegger et al.

ORGANIC LETTERS (2015)

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Article Chemistry, Organic

Cycloadditions of 1,2,3-Triazines Bearing C5-Electron Donating Substituents: Robust Pyrimidine Synthesis

Christopher M. Glinkerman et al.

ORGANIC LETTERS (2015)

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Article Chemistry, Organic

Synthesis of Quinolines from Allylic Alcohols via Iridium-Catalyzed Tandem Isomerization/Cyclization Combined with Potassium Hydroxide

Shu-jie Chen et al.

SYNTHESIS-STUTTGART (2015)

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Article Chemistry, Organic

An improved method for the regioselective synthesis of highly substituted quinolines from Morita-Baylis-Hillman adducts

Lucas A. Zeoly et al.

TETRAHEDRON LETTERS (2015)

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Article Chemistry, Organic

Synthesis of 2-substituted quinolines from alcohols

Xuefeng Xu et al.

TETRAHEDRON LETTERS (2015)

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Review Chemistry, Multidisciplinary

\ Metal-free domino one-pot protocols for quinoline synthesis

Jaideep B. Bharate et al.

RSC ADVANCES (2015)

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Review Chemistry, Multidisciplinary

Metal-Free Multicomponent Syntheses of Pyridines

Christophe Allais et al.

CHEMICAL REVIEWS (2014)

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Article Pharmacology & Pharmacy

Ceritinib: First Global Approval

Sohita Dhillon et al.

DRUGS (2014)

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Review Pharmacology & Pharmacy

Pazopanib: A Review of Its Use in the Management of Advanced Renal Cell Carcinoma

Paul L. McCormack

DRUGS (2014)

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Article Chemistry, Medicinal

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among US FDA Approved Pharmaceuticals

Edon Vitaku et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

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Letter Medicine, General & Internal

Ceritinib in ALK-Rearranged Non-Small-Cell Lung Cancer

Liang Shen et al.

NEW ENGLAND JOURNAL OF MEDICINE (2014)

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Article Chemistry, Organic

Highly Functionalized Pyridines Synthesis from N-Sulfonyl Ketimines and Alkynes Using the N-S Bond as an Internal Oxidant

Qian-Ru Zhang et al.

ORGANIC LETTERS (2014)

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Article Chemistry, Organic

Cycloadditions of Noncomplementary Substituted 1,2,3-Triazines

Erin D. Anderson et al.

ORGANIC LETTERS (2014)

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Article Chemistry, Organic

One-Step Synthesis of Quinolines via Palladium-Catalyzed Cross-Coupling of Cyclopropanols with Unprotected ortho-Bromoanilines

Andrei Nikolaev et al.

SYNLETT (2014)

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Article Chemistry, Organic

Copper-catalyzed domino reaction between 1-(2-halophenyl) methanamines and amidines or imidates for the synthesis of 2-substituted quinazolines

Mohamed A. Omar et al.

TETRAHEDRON (2014)

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Review Endocrinology & Metabolism

Overview and Management of Dermatologic Events Associated with Targeted Therapies for Medullary Thyroid Cancer

Mario E. Lacouture et al.

THYROID (2014)

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Article Chemistry, Organic

Copper-Catalyzed Sequential N-Arylation and Aerobic Oxidation: Synthesis of Quinazoline Derivatives

Qing Liu et al.

SYNLETT (2013)

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Article Cell Biology

Apoptosis of osteosarcoma cultures by the combination of the cyclin-dependent kinase inhibitor SCH727965 and a heat shock protein 90 inhibitor

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CELL DEATH & DISEASE (2013)

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Article Chemistry, Multidisciplinary

Copper-Catalyzed Synthesis of Quinazolines in Water Starting from o-Bromobenzylbromides and Benzamidines

Chandi C. Malakar et al.

CHEMISTRY-A EUROPEAN JOURNAL (2012)

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Article Chemistry, Organic

CuCl/DABCO/4-HO-TEMPO-Catalyzed Aerobic Oxidative Synthesis of 2-Substituted Quinazolines and 4H-3,1-Benzoxazines

Bing Han et al.

JOURNAL OF ORGANIC CHEMISTRY (2012)

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Article Chemistry, Organic

Stereoselective and Catalytic Access to β-Enaminones: An Entry to Pyrimidines

Eric Gayon et al.

JOURNAL OF ORGANIC CHEMISTRY (2012)

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Article Chemistry, Organic

Synthesis of Pyridines from Ketoximes and Terminal Alkynes via C-H Bond Functionalization

Rhia M. Martin et al.

JOURNAL OF ORGANIC CHEMISTRY (2012)

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Article Medicine, General & Internal

Pazopanib for metastatic soft-tissue sarcoma (PALETTE): a randomised, double-blind, placebo-controlled phase 3 trial

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LANCET (2012)

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Article Medicine, General & Internal

Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial

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Article Chemistry, Organic

CYCLOCONDENSATION OF 2-IODOBENZALDEHYDE WITH BENZAMIDINES CATALYZED BY COPPER(I) IODIDE: A ROUTE TO 2-ARYLQUINAZOLINES

A. V. Vypolzov et al.

CHEMISTRY OF HETEROCYCLIC COMPOUNDS (2011)

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Review Oncology

Pazopanib: Clinical development of a potent anti-angiogenic drug

Fabio A. B. Schutz et al.

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2011)

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Article Chemistry, Multidisciplinary

Inverse Electron Demand Diels-Alder Reactions of 1,2,3-Triazines: Pronounced Substituent Effects on Reactivity and Cycloaddition Scope

Erin D. Anderson et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2011)

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Article Chemistry, Organic

Scope of the Inverse Electron Demand Diels-Alder Reactions of 1,2,3-Triazine

Erin D. Anderson et al.

ORGANIC LETTERS (2011)

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Article Chemistry, Organic

An Improved Larock Synthesis of Quinolines via a Heck Reaction of 2-Bromoanilines and Allylic Alcohols

Matthew T. Stone

ORGANIC LETTERS (2011)

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Article Chemistry, Organic

Copper(II)-Catalyzed Synthesis of Pyrimidines from Propargylic Alcohols and Amidine: A Propargylation-Cyclization-Oxidation Tandem Reaction

Min Lin et al.

SYNLETT (2011)

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Article Chemistry, Organic

Copper-Catalyzed Synthesis of Quinazoline Derivatives via Ullmann-Type Coupling and Aerobic Oxidation

Chen Wang et al.

JOURNAL OF ORGANIC CHEMISTRY (2010)

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Article Biochemistry & Molecular Biology

A truncated minimal-E1a gene with potency to support adenoviral replication mediates antitumor activity by down-regulating Neu expression and preserving Rb function

Lin Fang et al.

CHEMICO-BIOLOGICAL INTERACTIONS (2009)

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Article Chemistry, Organic

Synthesis of Densely Substituted Pyrimidine Derivatives

Omar K. Ahmad et al.

JOURNAL OF ORGANIC CHEMISTRY (2009)

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Article Chemistry, Organic

Quinoline formation via a modified Combes reaction: examination of kinetics, substituent effects, and mechanistic pathways

Joseph C. Sloop

JOURNAL OF PHYSICAL ORGANIC CHEMISTRY (2009)

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Article Chemistry, Organic

Barium manganate in microwave-assisted oxidation reactions: synthesis of solvatochromic 2,4,6-triarylpyrimidines

Mark C. Bagley et al.

TETRAHEDRON LETTERS (2009)

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Article Chemistry, Multidisciplinary

Diverse reactions of 1,4-dilithio-1,3-dienes with nitriles: Facile access to tricyclic Delta(1)-bipyrrolines, multiply substituted pyridines, siloles, and (Z,Z)-Dienylsilanes by tuning of substituents on the butadienyl skeleton

Nan Yu et al.

CHEMISTRY-A EUROPEAN JOURNAL (2008)

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Review Chemistry, Organic

Advances in the syntheses of quinoline and quinoline-annulated ring systems

Sudharshan Madapa et al.

CURRENT ORGANIC CHEMISTRY (2008)

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Article Chemistry, Multidisciplinary

Synthesis of dihydropyridines and pyridines from Imines and alkynes via C-H activation

Denise A. Colby et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2008)

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Article Chemistry, Multidisciplinary

A simple, modular synthesis of substituted pyridines

Songbai Liu et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2008)

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Article Chemistry, Organic

Rhodium-catalyzed one-pot synthesis of substituted pyridine derivatives from α,β-unsaturated ketoximes and alkynes

Kanniyappan Parthasarathy et al.

ORGANIC LETTERS (2008)

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Article Chemistry, Multidisciplinary

Single-step synthesis of pyrimidine derivatives

Mohammad Movassaghi et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2006)

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Article Biochemistry & Molecular Biology

Differential induction of Leishmania donovani bi-subunit topoisomerase I-DNA cleavage complex by selected flavones and camptothecin: activity of flavones against camptothecin-resistant topoisomerase I

BB Das et al.

NUCLEIC ACIDS RESEARCH (2006)

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Article Chemistry, Organic

Improved methodologies for the preparation of highly substituted pyridines

YF Sainz et al.

JOURNAL OF ORGANIC CHEMISTRY (2005)

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Article Oncology

Expression of transforming growth factor-beta-1 and p27Kip1 in pancreatic adenocarcinomas:: relation with cell-cycle-associated proteins and clinicopathologic characteristics -: art. no. 98

N Culhaci et al.

BMC CANCER (2005)

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Article Chemistry, Organic

De novo synthesis of substituted pyridines

GD Henry

TETRAHEDRON (2004)

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Article Medicine, General & Internal

Membrane transport of camptothecin: facilitation by human P-glycoprotein (ABCB1) and multidrug resistance protein 2 (ABCC2)

Anita K. Lalloo et al.

BMC MEDICINE (2004)

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Article Chemistry, Multidisciplinary

Novel cycloaddition of nitriles with monolithio- and dilithiobutadienes

JL Chen et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2002)

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Article Chemistry, Organic

Novel facile synthesis of 2,2,4 substituted 1,2-dihydroquinolines via a modified Skraup reaction

ME Theoclitou et al.

TETRAHEDRON LETTERS (2002)

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