4.6 Review

Indol-3-ylglyoxylamide as Privileged Scaffold in Medicinal Chemistry

Related references

Note: Only part of the references are listed.
Review Biochemistry & Molecular Biology

Target-Based Anticancer Indole Derivatives for the Development of Anti-Glioblastoma Agents

Silvia Salerno et al.

Summary: Glioblastoma (GBM) is a highly aggressive and common primary brain tumor with a poor prognosis and high mortality rate. Current treatment options, including surgical resection, radiotherapy, and chemotherapy, have limited efficacy. This review focuses on the therapeutic benefits and clinical development of novel indole-based derivatives as potential anti-GBM agents. It discusses the current pre-clinical and clinical stage compounds, emphasizing the recent advances between 2013 and 2022. The mechanisms of action, such as protein kinase, tubulin, and p53 pathway inhibition, are also analyzed.

MOLECULES (2023)

Article Biochemistry & Molecular Biology

Piperazine-derived small molecules as potential Flaviviridae NS3 protease inhibitors. In vitro antiviral activity evaluation against Zika and Dengue viruses

Maria del Rosario Garcia-Lozano et al.

Summary: Since 2011, direct acting antiviral (DAAs) drugs have been approved for clinical use in HCV therapies, targeting different non-structural viral proteins. However, there is currently no licensed therapeutics for flavivirus infections, and the existing DENV vaccine, Dengvaxia, is limited to patients with preexisting DENV immunity. In this study, a library of 34 piperazine-derived small molecules was developed as potential inhibitors of flaviviridae NS3 protease, with two lead compounds showing promising activity against ZIKV and DENV.

BIOORGANIC CHEMISTRY (2023)

Article Biochemistry & Molecular Biology

Synthesis and cytotoxicity evaluation of DNA-interactive beta-carboline indolyl-3-glyoxamide derivatives: Topo-II inhibition and in silico modelling studies

Jay Prakash Soni et al.

Summary: In this study, a series of new beta-carboline tethered indole-3-glyoxylamide derivatives were synthesized, which showed significant pharmacological properties and prominent cytotoxicity. The compounds exhibited remarkable cytotoxicity against human cancer cell lines, especially melanoma, and showed selective toxicity towards cancer cells compared to normal cells. The compounds induced apoptosis and showed potential as DNA binders and inhibitors of Topoisomerase II. Molecular modeling studies confirmed their excellent DNA intercalation potential. In addition, in silico analysis predicted the promising drug-like properties of the synthesized derivatives.

BIOORGANIC CHEMISTRY (2023)

Article Biochemistry & Molecular Biology

The human microglial surveillant phenotype is preserved by de novo neurosteroidogenesis through the control of cholesterol homeostasis: Crucial role of 18 kDa Translocator Protein

Elisa Angeloni et al.

Summary: Neurodegenerative disease-associated microglia commonly exhibit harmful cholesterol accumulation, impairing their ability to resolve neuroinflammation. Neurosteroids, as potent anti-inflammatory molecules, play a crucial role in maintaining the immune surveillance phenotype of microglia. This study investigated the impact of neurosteroidogenesis on cholesterol homeostasis in a human microglia model, revealing the critical role of TSPO-mediated neurosteroidogenesis in regulating cholesterol trafficking. Pharmacological stimulation of TSPO enhanced cholesterol turnover and preserved a healthy immune surveillant phenotype, while TSPO knock-down led to excessive cholesterol accumulation and a dysfunctional phenotype.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE (2023)

Article Neurosciences

Translocator Protein Ligand PIGA1138 Reduces Disease Symptoms and Severity in Experimental Autoimmune Encephalomyelitis Model of Primary Progressive Multiple Sclerosis

Chiara Tremolanti et al.

Summary: Research suggests that phenylindoleglyoxylamydes (PIGAs) translocator protein (TSPO) ligands may have therapeutic potential in mice with myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) that mimics primary progressive multiple sclerosis (PPMS) in humans. Treatment with PIGA1138 significantly reduced clinical symptoms and improved motor function in MOG-EAE mice, while preserving myelin and axonal integrity. PIGA1138 also inhibited immune cell infiltration, reducing inflammation, and increased anti-inflammatory cytokine levels.

MOLECULAR NEUROBIOLOGY (2022)

Article Biochemistry & Molecular Biology

BPR0C261, An Analogous of Microtubule Disrupting Agent D-24851 Enhances the Radiosensitivity of Human Non-Small Cell Lung Cancer Cells via p53-Dependent and p53-Independent Pathways

Jyh-Der Leu et al.

Summary: BPR0C261 demonstrates dose-dependent cytotoxicity on A549 and H1299 cells, inducing maximum G2/M phase arrest and apoptosis in both cell lines. The combination of low concentration of BPR0C261 and X-rays shows a synergistic radiosensitizing effect on NSCLC cells.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Article Clinical Neurology

Epidemiology of Insomnia Prevalence, Course, Risk Factors, and Public Health Burden

Charles M. Morin et al.

SLEEP MEDICINE CLINICS (2022)

Article Biochemistry & Molecular Biology

Targeting TSPO Reduces Inflammation and Apoptosis in an In Vitro Photoreceptor-Like Model of Retinal Degeneration

Francesca Corsi et al.

Summary: TSPO plays an important role in neuropathologies and brain injury. The study found that by inhibiting inflammatory and apoptotic processes, as well as reducing LPS-induced cellular cytotoxicity, targeting TSPO has potential for therapeutic treatment of inflammatory-based retinal neurodegeneration.

ACS CHEMICAL NEUROSCIENCE (2022)

Review Chemistry, Medicinal

An update into the medicinal chemistry of translocator protein (TSPO) ligands

Elisabetta Barresi et al.

Summary: TSPO, a well-conserved protein in cells, plays crucial roles in cell functions and is associated with various diseases. High TSPO expression is linked to cancer, neuroinflammation, and brain injury, while low TSPO expression is associated with anxiety disorders. Therefore, TSPO is not only a potential drug target but also an effective diagnostic marker for related diseases.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Radiology, Nuclear Medicine & Medical Imaging

Cellular sources of TSPO expression in healthy and diseased brain

Erik Nutma et al.

Summary: TSPO, located in the outer mitochondrial membrane, is considered an in vivo marker of neuroinflammation as measured with PET. Changes in TSPO expression are observed in neurodegenerative, neuroinflammatory, and neuropsychiatric diseases, but further studies are needed to fully understand its cellular underpinnings and functional significance.

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2021)

Article Biochemistry & Molecular Biology

Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters

Elisabetta Barresi et al.

Summary: The study investigated compounds with chemical similarity to known PAMs of A(2B) AR, identifying lead compounds with potential as anti-osteoporosis agents. Further characterization of benzofurane derivative 9 confirmed its role as a PAM of A(2B) AR.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2021)

Review Biochemistry & Molecular Biology

Targeting metastatic cancer

Karuna Ganesh et al.

Summary: Improved understanding of metastases biology has led to advancements in targeting and treating both micro- and macrometastases. Recent studies have identified the unique biology of metastasis-initiating cells, providing new opportunities for developing more effective treatment strategies through cancer sequencing, mechanistic studies, and clinical trials. These insights offer potential for better outcomes in targeting metastatic relapse and improving patient survival.

NATURE MEDICINE (2021)

Article Chemistry, Medicinal

Synthesis, Structure-Activity Relationships, and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease

Shenyou Nie et al.

Summary: A novel series of compounds are found to be potent allosteric inhibitors of Zika virus protease, with inhibitory activities against homologous proteases of dengue and West Nile viruses as well. The most potent compounds showed strong inhibition of Zika virus replication in cells and in a mouse model, representing potential leads for drug development against Flavivirus infections.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Medicine, Research & Experimental

Recent trends in cancer therapy: A review on the current state of gene delivery

Esam Bashir Yahya et al.

Summary: Cancer treatment has always been a critical issue in clinical practice, with gene therapy showing potential to revolutionize the way different types of cancer are treated. Various approaches, such as targeting microRNAs and CRISPR/Cas9, have been developed for cancer gene therapy. Current research is focusing on exploring different strategies for cancer gene therapy.

LIFE SCIENCES (2021)

Article Biochemistry & Molecular Biology

De novo Neurosteroidogenesis in Human Microglia: Involvement of the 18 kDa Translocator Protein

Lorenzo Germelli et al.

Summary: Recent research has demonstrated that de novo neurosteroidogenesis occurs in human microglia, and the function of TSPO can influence this process, leading to increased release of BDNF mediated by neurosteroids.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

Article Chemistry, Medicinal

The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities

Marco Robello et al.

Summary: Researchers have utilized the α-ketoamide motif to design innovative hit/lead molecules tailored to a variety of biological targets, showing clinical potential for treating various pathological conditions. This perspective provides insights into the versatility of this chemical moiety as a privileged structure in drug discovery, highlighting its application as either a nonreactive or reactive moiety in compound design.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Pharmacology & Pharmacy

Cinnamic acid inhibits Zika virus by inhibiting RdRp activity

Yuting Chen et al.

Summary: Recent study showed that cinnamic acid possesses antiviral properties against Zika virus (ZIKV) and may serve as a potential effective anti-ZIKV drug by inhibiting the post-entry stage of the replication cycle, reducing mortality of mice, and viral load in the blood.

ANTIVIRAL RESEARCH (2021)

Article Chemistry, Medicinal

Quinoline and Quinazoline Derivatives Inhibit Viral RNA Synthesis by SARS-CoV-2 RdRp

Jianyuan Zhao et al.

Summary: Three compounds were identified to exhibit remarkable potency in inhibiting RNA synthesis driven by SARS-CoV-2 RdRp, showing potential for drug development against COVID-19.

ACS INFECTIOUS DISEASES (2021)

Article Biochemistry & Molecular Biology

Carbonic anhydrase activation profile of indole-based derivatives

Elisabetta Barresi et al.

Summary: Carbonic Anhydrase Activators (CAAs) may offer a new approach to treat conditions such as Alzheimer's disease, with promising selectivity towards specific isoforms. These activators have shown potential in enhancing spatial learning and memory therapy.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2021)

Article Chemistry, Inorganic & Nuclear

Two mixed valence diruthenium(ii,iii) isomeric complexes show different anticancer properties

Elisabetta Barresi et al.

Summary: The nature of ligands in Ru-2(ii,iii) paddlewheel complexes significantly influences their anticancer properties, with [Ru-2(EB776)(4)Cl] showing higher activity against a glioblastoma model compared to its isomer [Ru-2(EB106)(4)Cl]. These differences are attributed to steric hindrance, allowed conformations of the complexes, and the presence of hydrophilic regions in [Ru-2(EB776)(4)Cl], resulting in lower steric protection.

DALTON TRANSACTIONS (2021)

Article Chemistry, Medicinal

Design, synthesis and discovery of andrographolide derivatives against Zika virus infection

Feng Li et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Biochemistry & Molecular Biology

Mechanisms of Multidrug Resistance in Cancer Chemotherapy

Karol Bukowski et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Review Pharmacology & Pharmacy

Inhaled Phosphodiesterase 4 (PDE4) Inhibitors for Inflammatory Respiratory Diseases

Jonathan E. Phillips

FRONTIERS IN PHARMACOLOGY (2020)

Review Biochemistry & Molecular Biology

Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets

Sabrina Taliani et al.

MOLECULES (2020)

Article Medicine, General & Internal

Fostemsavir in Adults with Multidrug-Resistant HIV-1 Infection

Michael Kozal et al.

NEW ENGLAND JOURNAL OF MEDICINE (2020)

Review Biochemistry & Molecular Biology

Cinnamic Acid Derivatives and Their Biological Efficacy

Ngonidzashe Ruwizhi et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Article Biochemistry & Molecular Biology

Structure-activity relationships in a series of auranofin analogues showing remarkable antiproliferative properties

Ida Landini et al.

JOURNAL OF INORGANIC BIOCHEMISTRY (2020)

Review Biochemistry & Molecular Biology

Indole - a promising pharmacophore in recent antiviral drug discovery

Atukuri Dorababu

RSC MEDICINAL CHEMISTRY (2020)

Article Biochemistry & Molecular Biology

6-Bromoindolglyoxylamido derivatives as antimicrobial agents and antibiotic enhancers

Steven A. Li et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines

Melissa M. Cadelis et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir

Nicholas A. Meanwell et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Infectious Diseases

A quinoline compound inhibits the replication of dengue virus serotypes 1-4 in Vero cells

Hemalatha Beesetti et al.

ANTIVIRAL THERAPY (2018)

Editorial Material Biochemistry & Molecular Biology

Translocator protein and steroidogenesis

Barbara Costa et al.

BIOCHEMICAL JOURNAL (2018)

Review Chemistry, Inorganic & Nuclear

The side effects of platinum-based chemotherapy drugs: a review for chemists

Rabbab Oun et al.

DALTON TRANSACTIONS (2018)

Review Chemistry, Medicinal

Carbonic anhydrase activators

Claudiu T. Supuran

FUTURE MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Antiviral Activity of Novel Quinoline Derivatives against Dengue Virus Serotype 2

Carolina de la Guardia et al.

MOLECULES (2018)

Review Neurosciences

GABA(A) receptor: Positive and negative allosteric modulators

Richard W. Olsen

NEUROPHARMACOLOGY (2018)

Review Pharmacology & Pharmacy

The Benzodiazepine Binding Sites of GABAA Receptors

Erwin Sigel et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2018)

Article Chemistry, Medicinal

Synthesis of C5-tethered indolyl-3-glyoxylamide derivatives as tubulin polymerization inhibitors

Sravanthi Devi Guggilapu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Chemistry, Medicinal

2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine

Giselle Barbosa-Limaa et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Chemistry, Medicinal

Synthesis of thiazole linked indolyl-3-glyoxylamide derivatives as tubulin polymerization inhibitors

Sravanthi Devi Guggilapu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Biochemistry & Molecular Biology

Crystal structures of trimeric HIV envelope with entry inhibitors BMS-378806 and BMS-626529

Marie Pancera et al.

NATURE CHEMICAL BIOLOGY (2017)

Article Pharmacology & Pharmacy

Antiviral activities of selected antimalarials against dengue virus type 2 and Zika virus

Anuradha Balasubramanian et al.

ANTIVIRAL RESEARCH (2017)

Article Chemistry, Medicinal

Sequential one-pot synthesis of bis(indolyl)glyoxylamides: Evaluation of antibacterial and anticancer activities

Mukund P. Tantak et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016)

Review Chemistry, Multidisciplinary

The Next Generation of Platinum Drugs: Targeted Pt(II) Agents, Nanoparticle Delivery, and Pt(IV) Prodrugs

Timothy C. Johnstone et al.

CHEMICAL REVIEWS (2016)

Article Pharmacology & Pharmacy

TSPO-ligands prevent oxidative damage and inflammatory response in C6 glioma cells by neurosteroid synthesis

Anna Santoro et al.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2016)

Article Chemistry, Multidisciplinary

Synthesis and biological evaluation of novel carbazolyl glyoxamides as anticancer and antibacterial agents

Venkataramana P. O. Reddy et al.

RSC ADVANCES (2016)

Article Multidisciplinary Sciences

TSPO ligand residence time: a new parameter to predict compound neurosteroidogenic efficacy

Barbara Costa et al.

SCIENTIFIC REPORTS (2016)

Article Biochemistry & Molecular Biology

TSPO PIGA Ligands Promote Neurosteroidogenesis and Human Astrocyte Well-Being

Eleonora Da Pozzo et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2016)

Article Chemistry, Medicinal

2-(3′-Indolyl)-N-arylthiazole-4-carboxamides: Synthesis and evaluation of antibacterial and anticancer activities

Mukund P. Tantak et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Review Pharmacology & Pharmacy

Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors

Michael Juchum et al.

DRUG RESISTANCE UPDATES (2015)

Article Biochemistry & Molecular Biology

Cinnamic Acid and Cinnamaldehyde Ameliorate Cisplatin-Induced Splenotoxicity in Rats

Ola M. Abd El-Raouf et al.

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY (2015)

Article Chemistry, Medicinal

Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides

Elisabetta Barresi et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Microbiology

Novel Dengue Virus NS2B/NS3 Protease Inhibitors

Hongmei Wu et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2015)

Article Biochemistry & Molecular Biology

Allosteric modulators of human A2B adenosine receptor

Maria Letizia Trincavelli et al.

BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS (2014)

Article Biochemistry & Molecular Biology

Osteoblast differentiation and survival: A role for A2B adenosine receptor allosteric modulators

Maria Letizia Trincavelli et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH (2014)

Article Medicine, General & Internal

Varespladib and Cardiovascular Events in Patients With an Acute Coronary Syndrome The VISTA-16 Randomized Clinical Trial

Stephen J. Nicholls et al.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2014)

Article Chemistry, Medicinal

New Ianthelliformisamine Derivatives as Antibiotic Enhancers against Resistant Gram-Negative Bacteria

Cyril Pieri et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Chemistry, Organic

Synthesis and biological activity of novel bis-indole inhibitors of bacterial transcription initiation complex formation

Marcin Mielczarek et al.

ORGANIC & BIOMOLECULAR CHEMISTRY (2014)

Article Oncology

BPR0C305, an orally active microtubule-disrupting anticancer agent

Wen-Tai Li et al.

ANTI-CANCER DRUGS (2013)

Article Biochemistry & Molecular Biology

Neuronal carbonic anhydrase VII provides GABAergic excitatory drive to exacerbate febrile seizures

Eva Ruusuvuori et al.

EMBO JOURNAL (2013)

Article Chemistry, Medicinal

Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives

Sabrina Taliani et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Pharmacology & Pharmacy

Retro peptide-hybrids as selective inhibitors of the Dengue virus NS2B-NS3 protease

Christoph Nitsche et al.

ANTIVIRAL RESEARCH (2012)

Review Chemistry, Medicinal

Recent Developments in Potential Anxiolytic Agents Targeting GABAA/BzR Complex or the Translocator Protein (18kDa) (TSPO)

Caroline Nothdurfter et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2012)

Review Endocrinology & Metabolism

Translocator Protein (18 kDa) as a Target for Novel Anxiolytics with a Favourable Side-Effect Profile

C. Nothdurfter et al.

JOURNAL OF NEUROENDOCRINOLOGY (2012)

Review Pharmacology & Pharmacy

Anxioselective anxiolytics: on a quest for the Holy Grail

Phil Skolnick

TRENDS IN PHARMACOLOGICAL SCIENCES (2012)

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of α-ketoamides as inhibitors of the Dengue virus protease with antiviral activity in cell-culture

Christian Steuer et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2011)

Article Biochemistry & Molecular Biology

Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases

Christoph Nitsche et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2011)

Article Chemistry, Medicinal

Synthesis and evaluation of indole-based new scaffolds for antimicrobial activities-Identification of promising candidates

Palwinder Singh et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2011)

Article Biochemistry & Molecular Biology

Designed Multiple Ligands for Cancer Therapy

N. M. O'Boyle et al.

CURRENT MEDICINAL CHEMISTRY (2011)

Article Multidisciplinary Sciences

Activation of p53 by Nutlin-3a Induces Apoptosis and Cellular Senescence in Human Glioblastoma Multiforme

Ruth Villalonga-Planells et al.

PLOS ONE (2011)

Article Chemistry, Medicinal

Synthesis and biological evaluation of indolyl glyoxylamides as a new class of antileishmanial agents

Shikha S. Chauhan et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)

Article Chemistry, Medicinal

Synthesis of 2-(pyrimidin-2-yl)-1-phenyl-2,3,4,9-tetrahydro-1H-β-carbolines as antileishmanial agents

Ravi Kumar et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)

Editorial Material Pharmacology & Pharmacy

Varespladib methyl in cardiovascular disease

Robert S. Rosenson et al.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2010)

Article Chemistry, Medicinal

Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns

Nicholas A. Meanwell et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

Review Chemistry, Inorganic & Nuclear

Metal complexes involving indole rings: Structures and effects of metal-indole interactions

Yuichi Shimazaki et al.

COORDINATION CHEMISTRY REVIEWS (2009)

Review Biochemistry & Molecular Biology

Translocator Protein Ligands as Promising Therapeutic Tools for Anxiety Disorders

S. Taliani et al.

CURRENT MEDICINAL CHEMISTRY (2009)

Article Chemistry, Medicinal

Selective p38α Inhibitors Clinically Evaluated for the Treatment of Chronic Inflammatory Disorders

David M. Goldstein et al.

JOURNAL OF MEDICINAL CHEMISTRY (2009)

Review Chemistry, Medicinal

From Nature to Drug Discovery: The Indole Scaffold as a 'Privileged Structure'

Fernando Rodrigues de Sa Alves et al.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2009)

Review Chemistry, Medicinal

HIV Entry Inhibitors and Their Potential in HIV Therapy

Keduo Qian et al.

MEDICINAL RESEARCH REVIEWS (2009)

Article Multidisciplinary Sciences

Demonstration of Genetic Exchange During Cyclical Development of Leishmania in the Sand Fly Vector

Natalia S. Akopyants et al.

SCIENCE (2009)

Review Rheumatology

How Antirheumatic Drugs Protect Joints From Damage in Rheumatoid Arthritis

Georg Schett et al.

ARTHRITIS AND RHEUMATISM (2008)

Article Chemistry, Medicinal

Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents

Mohamed Takhi et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)

Article Pharmacology & Pharmacy

Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity

Ronald J. Hill et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2008)

Review Clinical Neurology

Prion proteins:: Physiological functions and role in neurological disorders

Wei Hu et al.

JOURNAL OF THE NEUROLOGICAL SCIENCES (2008)

Review Biotechnology & Applied Microbiology

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

Claudiu T. Supuran

NATURE REVIEWS DRUG DISCOVERY (2008)

Review Rheumatology

The p38 mitogen-activated protein kinase (MAPK) pathway in rheumatoid arthritis

G. Schett et al.

ANNALS OF THE RHEUMATIC DISEASES (2008)

Article Chemistry, Medicinal

Synthesis of marine alkaloid: 8,9-dihydrocoscinamide B and its analogues as Novel class of antileishmanial agents

Leena Gupta et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2007)

Review Dentistry, Oral Surgery & Medicine

p38 pathway kinases as anti-inflammatory drug targets

J. F. Schindler et al.

JOURNAL OF DENTAL RESEARCH (2007)

Review Biochemistry & Molecular Biology

GABA(A)/Bz receptor subtypes as targets for selective drugs

F. Da Settimo et al.

CURRENT MEDICINAL CHEMISTRY (2007)

Review Chemistry, Medicinal

P38 mitogen-activated protein kinase (MAPK) in rheumatoid arthritis

J. Westra et al.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2006)

Article Chemistry, Medicinal

Syntheses of new substituted triazino tetrahydroisoquinolines and beta-carbolines as novel antileishmanial agents

A Kumar et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2006)

Article Immunology

The global status of resistance to antiretroviral drugs

S Vella et al.

CLINICAL INFECTIOUS DISEASES (2005)

Article Biochemistry & Molecular Biology

BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo

Y Kuma et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2005)

Review Pharmacology & Pharmacy

The benzodiazepine binding site of GABAA receptors as a target for the development of novel anxiolytics

JR Atack

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2005)

Review Biotechnology & Applied Microbiology

Cellular processing of platinum anticancer drugs

D Wang et al.

NATURE REVIEWS DRUG DISCOVERY (2005)

Review Public, Environmental & Occupational Health

Benefit-risk assessment of zaleplon in the treatment of insomnia

J Barbera et al.

DRUG SAFETY (2005)

Article Chemistry, Medicinal

Recognition of privileged structures by G-protein coupled receptors

K Bondensgaard et al.

JOURNAL OF MEDICINAL CHEMISTRY (2004)

Article Multidisciplinary Sciences

A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding

PF Lin et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2003)

Review Pharmacology & Pharmacy

The mouse light/dark box test

M Bourin et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2003)

Article Neurosciences

Anxioselective Compounds Acting at the GABA(A) Receptor Benzodiazepine Binding Site

John R. Atack

CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS (2003)

Review Public, Environmental & Occupational Health

New drugs for insomnia - Comparative tolerability of zopiclone, zolpidem and zaleplon

MG Terzano et al.

DRUG SAFETY (2003)

Article Infectious Diseases

Emerging linezolid-resistant Enterococcus faecalis and Enterococcus faecium isolated from two Austrian patients in the same intensive care unit

AP Johnson et al.

EUROPEAN JOURNAL OF CLINICAL MICROBIOLOGY & INFECTIOUS DISEASES (2002)

Article Biochemistry & Molecular Biology

Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

C Pargellis et al.

NATURE STRUCTURAL BIOLOGY (2002)

Review Pharmacology & Pharmacy

Recent advances in PDE4 inhibitors as immunoregulators and anti-inflammatory drugs

C Burnouf et al.

CURRENT PHARMACEUTICAL DESIGN (2002)

Article Pharmacology & Pharmacy

A new benzodiazepine pharmacology

H Mohler et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2002)

Review Oncology

Taxanes in combined modality therapy for solid tumors

H Choy

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2001)

Article Multidisciplinary Sciences

Surfing the p53 network

B Vogelstein et al.

NATURE (2000)

Article Pharmacology & Pharmacy

Linezolid

D Clemett et al.

DRUGS (2000)