Abstract
The sulfonamides constitute an important class of drugs, with several types of pharmacological agents possessing antibacterial, anti-carbonic anhydrase, diuretic, hypoglycaemic, antithyroid, protease inhibitory and anticancer activity among others. A recently developed class of pharmacological agents incorporating primary sulfamoyl moieties in their molecule is constituted by the COX-2 selective inhibitors, with at least two clinically used drugs, celecoxib and valdecoxib. Another drug of this class, rofecoxib, does not contain sulfonamide moieties, but the isosteric and isoelectronic methylsulfone group. It was recently shown that the sulfonamide COX-2 selective inhibitors (but not the methylsulfone ones) also act as nanomolar inhibitors of several isozymes of the metallo-enzyme carbonic anhydrase (CA), some of which are strongly involved in tumourigenesis. In consequence, the potent anticancer effects of the sulfonamide COX-2 selective inhibitors and the much weaker such effects of rofecoxib, reported ultimately by many researchers, may be explained by the contribution of CA inhibition to such processes in addition to COX-2 inhibition.
Keywords: COX-2, CA inhibition, methylsulfone, metallo-enzyme, carbonic anhydrase, tumourigenesis
Mini-Reviews in Medicinal Chemistry
Title: COX-2 Selective Inhibitors, Carbonic Anhydrase Inhibition and Anticancer Properties of Sulfonamides Belonging to This Class of Pharmacological Agents
Volume: 4 Issue: 6
Author(s): Claudiu T. Supuran, Angela Casini, Antonio Mastrolorenzo and Andrea Scozzafava
Affiliation:
Keywords: COX-2, CA inhibition, methylsulfone, metallo-enzyme, carbonic anhydrase, tumourigenesis
Abstract: The sulfonamides constitute an important class of drugs, with several types of pharmacological agents possessing antibacterial, anti-carbonic anhydrase, diuretic, hypoglycaemic, antithyroid, protease inhibitory and anticancer activity among others. A recently developed class of pharmacological agents incorporating primary sulfamoyl moieties in their molecule is constituted by the COX-2 selective inhibitors, with at least two clinically used drugs, celecoxib and valdecoxib. Another drug of this class, rofecoxib, does not contain sulfonamide moieties, but the isosteric and isoelectronic methylsulfone group. It was recently shown that the sulfonamide COX-2 selective inhibitors (but not the methylsulfone ones) also act as nanomolar inhibitors of several isozymes of the metallo-enzyme carbonic anhydrase (CA), some of which are strongly involved in tumourigenesis. In consequence, the potent anticancer effects of the sulfonamide COX-2 selective inhibitors and the much weaker such effects of rofecoxib, reported ultimately by many researchers, may be explained by the contribution of CA inhibition to such processes in addition to COX-2 inhibition.
Export Options
About this article
Cite this article as:
Supuran T. Claudiu, Casini Angela, Mastrolorenzo Antonio and Scozzafava Andrea, COX-2 Selective Inhibitors, Carbonic Anhydrase Inhibition and Anticancer Properties of Sulfonamides Belonging to This Class of Pharmacological Agents, Mini-Reviews in Medicinal Chemistry 2004; 4 (6) . https://dx.doi.org/10.2174/1389557043403792
DOI https://dx.doi.org/10.2174/1389557043403792 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Effect of DNA Repair Deficiencies on the Cytotoxicity of Drugs Used in Cancer Therapy - A Review
Current Medicinal Chemistry Immunotherapy of Human Cancers Using Gene Modified T Lymphocytes
Current Gene Therapy DNA Intercalators in Cancer Therapy: Organic and Inorganic Drugs and Their Spectroscopic Tools of Analysis
Mini-Reviews in Medicinal Chemistry Neuroprotective Gene Therapy for the Treatment of Inherited Retinal Degeneration
Current Gene Therapy Cytotoxicity and Target Modulation in Pediatric Solid Tumors by the Proteasome Inhibitor Carfilzomib
Current Cancer Drug Targets A Medicinal Chemist’s Perspective Towards Structure Activity Relationship of Heterocycle Based Anticancer Agents
Current Topics in Medicinal Chemistry Therapeutic Potential of microRNA Against Th2-associated Immune Disorders
Current Topics in Medicinal Chemistry Alkaloids from Cyanobacteria with Diverse Powerful Bioactivities
Mini-Reviews in Medicinal Chemistry Acute Myeloid Leukemia in the Elderly: Current Therapeutic Results and Perspectives for Clinical Research
Reviews on Recent Clinical Trials Refractory Chronic Lymphocytic Leukemia: A Therapeutic Challenge
Current Cancer Drug Targets An Overview of Notch Signaling in Adult Tissue Renewal and Maintenance
Current Alzheimer Research System Models, Assays and Endpoint Parameters to Evaluate Anticancer Compounds During Preclinical Screening
Current Medicinal Chemistry MicroRNAs in Tumorigenesis
Current Pharmaceutical Biotechnology Infrared-Spectroscopy: A Non-Invasive Tool for Medical Diagnostics and Drug Analysis
Current Medicinal Chemistry Myelodysplastic/Myeloproliferative Neoplasms
Current Cancer Therapy Reviews Recent Advances in Targeting Viral Proteases for the Discovery of Novel Antivirals
Current Topics in Medicinal Chemistry Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer
Current Medicinal Chemistry Common and Uncommon Features of Rheumatoid Arthritis and Chronic Obstructive Pulmonary Disease: Clues to a Future Therapy
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Bio-AIMS Collection of Chemoinformatics Web Tools based on Molecular Graph Information and Artificial Intelligence Models
Combinatorial Chemistry & High Throughput Screening Cellular and Molecular Networks in Chronic Myeloid Leukemia: The Leukemic Stem, Progenitor and Stromal Cell Interplay
Current Drug Targets