Abstract
Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and providing a new target for the development of COX-2-selective drugs without gastrointestinal side-effects. Keeping in view the importance of this pharmacological class, several literature reports have underlined the impact of these antiinflammatory compounds in therapeutics. The present review considers the most recently published literature concerning COX-2 inhibitors until 2016. Through a wide chemical classification, the last developments concerning this therapeutic family by highlighting structure-activity relationships insights and mechanisms are presented. A summary of the principal adverse effects observed and an overview of the new potential therapeutic indications for COX-2 inhibitors are also reported.
Keywords: COX-2 inhibitors, Inflammation, Non-steroidal anti-inflammatory Drugs, Cyclooxygenase, COX-1/COX-2 inhibition, Structure–activity relationship.
Current Topics in Medicinal Chemistry
Title:Update on COX-2 Selective Inhibitors: Chemical Classification, Side Effects and their Use in Cancers and Neuronal Diseases
Volume: 17 Issue: 26
Author(s): Anita-Marie Rayar, Nathalie Lagarde, Clotilde Ferroud , Jean-Francois Zagury, Matthieu Montes and Maite Sylla-Iyarreta Veitia*
Affiliation:
- Equipe de chimie moleculaire, Laboratoire de Chimie moleculaire, genie des procedes chimiques et energetiques, EA7341, Conservatoire national des arts et metiers, 2 rue Conte, 75003 Paris,France
Keywords: COX-2 inhibitors, Inflammation, Non-steroidal anti-inflammatory Drugs, Cyclooxygenase, COX-1/COX-2 inhibition, Structure–activity relationship.
Abstract: Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and providing a new target for the development of COX-2-selective drugs without gastrointestinal side-effects. Keeping in view the importance of this pharmacological class, several literature reports have underlined the impact of these antiinflammatory compounds in therapeutics. The present review considers the most recently published literature concerning COX-2 inhibitors until 2016. Through a wide chemical classification, the last developments concerning this therapeutic family by highlighting structure-activity relationships insights and mechanisms are presented. A summary of the principal adverse effects observed and an overview of the new potential therapeutic indications for COX-2 inhibitors are also reported.
Export Options
About this article
Cite this article as:
Rayar Anita-Marie , Lagarde Nathalie , Ferroud Clotilde , Zagury Jean-Francois , Montes Matthieu and Sylla-Iyarreta Veitia Maite*, Update on COX-2 Selective Inhibitors: Chemical Classification, Side Effects and their Use in Cancers and Neuronal Diseases, Current Topics in Medicinal Chemistry 2017; 17 (26) . https://dx.doi.org/10.2174/1568026617666170821124947
DOI https://dx.doi.org/10.2174/1568026617666170821124947 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Pathways Related to the Anti-Cancer Effects of Metabolites Derived from Cerrado Biome Native Plants: An Update and Bioinformatics Analysis on Oral Squamous Cell Carcinoma
Protein & Peptide Letters Progress of HDAC Inhibitor Panobinostat in the Treatment of Cancer
Current Drug Targets Development of Focal Adhesion Kinase Inhibitors in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Efficacy of Yun Zhi (Coriolus versicolor) on Survival in Cancer Patients: Systematic Review and Meta-Analysis
Recent Patents on Inflammation & Allergy Drug Discovery MicroRNAs Regulate the Epithelial to Mesenchymal Transition (EMT) in Cancer Progression
MicroRNA Preparation, Characterization and <i>In Vitro</i> Biological Evaluation of Novel Curcumin Derivatives as Cytotoxic and Apoptosis-Inducing Agents
Anti-Cancer Agents in Medicinal Chemistry From Test Tube to Clinical Trial; Promising Herbs with NF-κB and COX- 2 Activity
Current Immunology Reviews (Discontinued) Peptides for Diagnosis and Treatment of Colorectal Cancer
Current Medicinal Chemistry Pathobiology and Therapeutic Implications of Tumor Acidosis
Current Medicinal Chemistry Molecular Diversity of Seed-borne Fusarium Species Associated with Maize in India
Current Genomics Has Selenium a Chemopreventive Effect on Hepatocellular Carcinoma?
Mini-Reviews in Medicinal Chemistry MicroRNA-21: From Cancer to Cardiovascular Disease
Current Drug Targets Novel Oral Anticoagulants for Venous Thromboembolism with Special Emphasis on Risk of Hemorrhagic Complications and Reversal Agents
Current Drug Therapy Tyrosine Kinase Blockers: New Hope for Successful Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Metastasis-Inducing S100A4 Protein: Implication in Non-Malignant Human Pathologies
Current Molecular Medicine Monoclonal Antibodies as Cancer Therapeutics
Recent Patents on Biotechnology Perspectives for Novel Mixed Diruthenium-Organic Drugs as Metallopharmaceuticals in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Scorpion Toxin Polyptides as Therapeutic Agents: An Overview
Protein & Peptide Letters Domperidone and Long QT Syndrome
Current Drug Safety Nitric Oxide and the Regulation of Apoptosis in Tumour Cells
Current Pharmaceutical Design