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Article
Biochemistry & Molecular Biology
Luka Krstulovic et al.
Summary: New 7-chloro-4-aminoquinoline-benzimidazole compounds were synthesized and characterized. They showed strong cytotoxic activity and effectively suppressed cell cycle progression in leukemia and lymphoma cells. Compound 12d exhibited good solubility and permeability, bound to c-Src with high affinity, and could be a potential candidate for the development of antitumor drugs.
Review
Biochemistry & Molecular Biology
Beatriz G. G. de la Torre et al.
Summary: While the world was battling with the COVID-19 Omicron wave at the end of 2021, except for China, most countries ended 2022 with COVID-19 being treated like the flu. As a result, the U.S. Food and Drug Administration (FDA) only authorized 37 new drugs this year, compared to an average of 52 in the previous four years. This marks the second lowest number of drug approvals in the last six years, even though it may change in the future. The decrease in FDA approvals mainly applies to small molecule drugs, while biologics and TIDES have remained relatively constant.
Article
Oncology
Frankie A. Holmes et al.
Summary: ExteNET study showed that neratinib significantly improved invasive disease-free survival in women with early-stage HER2-positive breast cancer compared to placebo after 1 year of treatment with trastuzumab-based therapy. The final analysis revealed that overall survival rates were comparable between neratinib and placebo in the extended adjuvant setting.
EUROPEAN JOURNAL OF CANCER
(2023)
Review
Pharmacology & Pharmacy
Yeuan Ting Lee et al.
Summary: Cancer is a major global cause of death and a continuing threat to human health. Drug resistance is a significant challenge in cancer treatment, and developing new drugs targeting malignant cells is a high priority. Benzimidazole and its derivatives have shown potential as anticancer therapeutics through various mechanisms, making them an important focus in medicinal chemistry and biology. This review provides updates on the mechanisms and structure-activity relationships of benzimidazole derivatives, from conventional anticancer treatments to precision healthcare. (c) 2023 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
ACTA PHARMACEUTICA SINICA B
(2023)
Article
Multidisciplinary Sciences
James J. Harding et al.
Summary: In patients with biliary tract cancer, HER2 alterations correlate with poor prognosis. A phase II clinical trial showed that the tyrosine kinase inhibitor neratinib has some efficacy in treating advanced biliary tract cancers with HER2-mutation positive. The objective response rate to neratinib was 16% (95% CI 4.5-36.1%).
NATURE COMMUNICATIONS
(2023)
Review
Chemistry, Medicinal
Adarsh Kumar et al.
Summary: Cancer is a major healthcare challenge worldwide, calling for the development of safer and target-specific anticancer drugs. This study summarizes the use of nitrogen-containing heterocycles in cancer treatment, providing insights into their pharmacological properties and mechanisms of action.
Review
Chemistry, Medicinal
Mohammad Mahboob Alam
Summary: Recent advancements in 1,2,3-triazole hybrids have shown promising potential in the development of anticancer agents. These compounds exhibit remarkable biological potential and offer significant opportunities in combating cancer.
ARCHIV DER PHARMAZIE
(2022)
Article
Oncology
Rebecca L. Siegel et al.
Summary: Each year, the American Cancer Society compiles data on cancer occurrence and outcomes in the United States. The latest data shows that breast and prostate cancer progress has stagnated, while lung cancer has shown improvements in survival rates. Lung cancer incidence for advanced disease has declined while localized-stage rates have increased, resulting in higher survival rates. Mortality patterns align with incidence trends, with lung cancer deaths declining rapidly, breast cancer deaths slowing, and prostate cancer deaths stabilizing.
CA-A CANCER JOURNAL FOR CLINICIANS
(2022)
Review
Biochemistry & Molecular Biology
Beatriz G. de la Torre et al.
Summary: Similar to last year, 2021 will be remembered for the COVID-19 pandemic. Despite the approval of five vaccines, the pandemic remains uncontrolled. However, there have been significant drug approvals by the FDA, with 50 drugs authorized in 2021. Nitrogen aromatic heterocycles and fluorine atoms continue to be predominant among small molecules.
Review
Chemistry, Medicinal
Zohor Mohammad Mahdi Alzhrani et al.
Summary: Benzimidazole is a nitrogen-containing fused heterocycle that has been extensively explored in medicinal chemistry. It possesses various biological activities and some compounds have been approved for the treatment of diseases.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Lian-Shun Feng et al.
Summary: Benzimidazole derivatives have diverse anticancer properties, including interference with cell division, induction of apoptosis, and blockage of glucose transport. Benzimidazole hybrids can exhibit dual or multiple antiproliferative activities and have the potential to overcome drug resistance. This article provides a comprehensive landscape of benzimidazole hybrids as potential anticancer agents, discussing the structure-activity relationship and mechanisms of action.
ARCHIV DER PHARMAZIE
(2022)
Article
Oncology
Niamh Cunningham et al.
Summary: This study describes the tolerability and efficacy of neratinib as a monotherapy and in combination with capecitabine in advanced HER2-positive breast cancer. The results showed that neratinib was effective in both patients with and without brain metastases, with similar progression-free survival and overall survival rates as previous trials. Diarrhea was the most common adverse event but could be managed with prophylaxis. Routine anti-diarrheal prophylaxis allows this combination therapy to be safely delivered to patients in a real-world setting.
BREAST CANCER RESEARCH AND TREATMENT
(2022)
Review
Biochemistry & Molecular Biology
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)
Review
Chemistry, Multidisciplinary
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)
Review
Oncology
Talha Bin Emran et al.
Summary: This review discusses the mechanisms of multidrug resistance in cancer cells and explores methods to inhibit, circumvent, or reverse the development of multidrug resistance. It highlights the hypoxia- and autophagy-mediated resistance mechanisms and discusses other molecular and cellular mechanisms of drug resistance.
FRONTIERS IN ONCOLOGY
(2022)
Review
Pharmacology & Pharmacy
Deniz Lengerli et al.
Summary: The 1,2,3-triazole ring plays a significant role in medicinal chemistry due to its unique structural properties and synthetic versatility. Recent research suggests that the 1,2,3-triazole ring may have a prominent role in drug molecules, and further studies are needed to gain a deeper understanding of its role in molecular recognition.
EXPERT OPINION ON DRUG DISCOVERY
(2022)
Article
Multidisciplinary Sciences
Dumitrela Diaconu et al.
Summary: Two new classes of hybrid quinoline-imidazole/benzimidazole derivatives were designed and synthesized to evaluate their anticancer and antimicrobial activity. The results showed that certain compounds exhibited excellent nonselective or selective anticancer activity against different cancer cell lines, as well as good antimicrobial activity against Gram-negative bacteria and one compound against Gram-positive bacteria. These findings suggest that these compounds have the potential to be candidates for future drug development.
SCIENTIFIC REPORTS
(2022)
Review
Chemistry, Medicinal
Ankit Kumar Singh et al.
Summary: Cancer is a complex disease, and the efficacy of conventional anticancer drugs varies. The hybrid approach of combining two drugs into a single molecule shows potential in improving treatment efficacy and reducing drug resistance. Recent research has identified promising hybrid molecules with anticancer properties. This study provides valuable knowledge for researchers working on complex diseases like cancer.
Review
Biochemistry & Molecular Biology
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)
Review
Pharmacology & Pharmacy
Shalini et al.
Summary: The development of hybrid molecules in cancer chemotherapy has shown promising results, with many entering clinical trials or the drug market in recent years. The collaboration between chemistry, biology, and pharmacology has greatly contributed to the advancement of hybrid chemotherapeutics.
EXPERT OPINION ON DRUG DISCOVERY
(2021)
Review
Pharmacology & Pharmacy
Ruth Nussinov et al.
Summary: Driver mutations play a critical role in cancer initiation and progression, with drug resistance being a common challenge in pharmacological treatment. The emergence of drug resistance can be attributed to a variety of mechanisms, such as mutations occurring in the same or different proteins, and in the same or parallel pathways. The complexity of genetic alterations and tumor microenvironment changes poses challenges in predicting drug resistance and requires further research in precision medicine.
DRUG RESISTANCE UPDATES
(2021)
Article
Chemistry, Medicinal
Osama M. Soltan et al.
Summary: Protein kinases have emerged as crucial targets in cancer treatment, with the design of multi-target drugs showing potential to enhance efficacy, reduce side effects, and maintain pharmacokinetic properties. Hybrid drugs combining kinase inhibitors with conventional chemotherapeutics or targeted therapies present a new approach in cancer treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Beatriz G. de la Torre et al.
Summary: In 2020, a total of 53 new drugs were approved by the US FDA, including 40 new chemical entities and 13 biologics. The approved drugs consist of monoclonal antibodies, antibody-drug conjugates, peptides, and oligonucleotides, with a notable presence of fluorine atoms and/or nitrogen aromatic heterocycles. These new drugs are classified based on their chemical structures as biologics, TIDES, natural products, fluorine-containing molecules, nitrogen aromatic heterocycles, and other small molecules.
Article
Oncology
Hyuna Sung et al.
Summary: The global cancer burden in 2020 saw an estimated 19.3 million new cancer cases and almost 10.0 million cancer deaths. Female breast cancer surpassed lung cancer as the most commonly diagnosed cancer, while lung cancer remained the leading cause of cancer death. These trends are expected to rise in 2040, with transitioning countries experiencing a larger increase compared to transitioned countries due to demographic changes and risk factors associated with globalization and a growing economy. Efforts to improve cancer prevention measures and provision of cancer care in transitioning countries will be crucial for global cancer control.
CA-A CANCER JOURNAL FOR CLINICIANS
(2021)
Review
Chemistry, Medicinal
Christine S. W. Law et al.
Summary: Benzimidazole derivatives have been widely studied in the pharmaceutical field for their wide range of pharmacological activities. This review outlines their biological effects and mechanisms of action, highlighting their potential for clinical drug development. Additionally, the study discusses novel therapeutic approaches for different target diseases using patented benzimidazoles.
Review
Biochemistry & Molecular Biology
Jeremy C. Burton et al.
Summary: The MAPK p38 plays a crucial role in regulating responses to environmental stress and inflammation. A newly identified atypical p38 signaling pathway driven by direct interaction between TAB1 and p38α has been linked to various diseases including dermal and vascular inflammation, myocardial ischemia, and cancer metastasis. Further studies are needed to fully understand the implications and mechanisms of atypical p38 signaling.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Paulo Michel Pinheiro Ferreira et al.
Summary: Chloroquine and hydroxychloroquine are commonly used drugs for relieving acute and chronic inflammatory diseases, and they have shown potential in enhancing the efficacy of chemotherapy in cancer treatment. However, they may also contribute to drug resistance in cancer cells and have various antitumor mechanisms unrelated to autophagy. The link between these mechanisms, clinical efficacy, and pharmacological safety remains not fully understood.
PHARMACOLOGICAL RESEARCH
(2021)
Review
Pharmacology & Pharmacy
Ting Liang et al.
Summary: Recent advances in research on 1,2,3-triazole-containing compounds with anti-lung cancer potential have been significant, with discussions on their structure-activity relationship and mechanisms of action to facilitate the rational development of novel anti-lung cancer candidates.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Beatriz G. de la Torre et al.
Review
Biochemistry & Molecular Biology
Chih-Yeu Fang et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Meeting Abstract
Hematology
Katherine Tarlock et al.
Article
Oncology
Xiaoyan Si et al.
THERAPEUTIC ADVANCES IN MEDICAL ONCOLOGY
(2020)
Article
Oncology
Le Zhang et al.
INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS
(2019)
Review
Biochemistry & Molecular Biology
Beatriz G. de la Torre et al.
Review
Pharmacology & Pharmacy
Xiangyi Jiang et al.
EXPERT OPINION ON DRUG DISCOVERY
(2019)
Article
Oncology
Wen Wee Ma et al.
AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS
(2019)
Article
Multidisciplinary Sciences
Haijiao Zhang et al.
NATURE COMMUNICATIONS
(2019)
Article
Oncology
Antonio Omuro et al.
JOURNAL OF CLINICAL ONCOLOGY
(2018)
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Chemistry, Medicinal
Luka Krstulovic et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Toxicology
Daiying Zuo et al.
TOXICOLOGY IN VITRO
(2017)
Article
Multidisciplinary Sciences
Antoine Daina et al.
SCIENTIFIC REPORTS
(2017)
Article
Chemistry, Organic
Reham A. I. Abou-Elkhair et al.
Article
Chemistry, Medicinal
Kristina Starcevic et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2012)
Article
Biochemical Research Methods
Kai-Cheng Hsu et al.
BMC BIOINFORMATICS
(2011)
Article
Biochemistry & Molecular Biology
Eric M. Guantai et al.
BIOORGANIC & MEDICINAL CHEMISTRY
(2010)
Article
Biochemistry & Molecular Biology
Tian-Jun Zhou et al.
ACTA BIOCHIMICA ET BIOPHYSICA SINICA
(2006)
Article
Chemistry, Medicinal
DF Veber et al.
JOURNAL OF MEDICINAL CHEMISTRY
(2002)
Article
Biochemistry & Molecular Biology
Z Chen et al.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2001)
