Abstract
Microtubules are cytoskeletal components that play important roles in a number of cellular processes. Colchicine binding site inhibitors (CSIs) is one major class of tubulin polymerization inhibitors, inhibiting microtubule polymerization and blocking cell proliferation at metaphase during mitosis. Many CSIs were discovered or designed and synthesized as anticancer agents in the past several years and great progress had been made. Here, we discuss the insights gained so far relevant to the mechanism of CSIs and their common pharmacophore. The recent development of CSIs with their biological activity and structure-activity relationship (SAR) are also reviewed.
Keywords: Microtubules, colchicine binding site, inhibitor, SAR, anticancer
Mini-Reviews in Medicinal Chemistry
Title: Recent Development and SAR Analysis of Colchicine Binding Site Inhibitors
Volume: 9 Issue: 10
Author(s): Jing Chen, Tao Liu, Xiaowu Dong and Yongzhou Hu
Affiliation:
Keywords: Microtubules, colchicine binding site, inhibitor, SAR, anticancer
Abstract: Microtubules are cytoskeletal components that play important roles in a number of cellular processes. Colchicine binding site inhibitors (CSIs) is one major class of tubulin polymerization inhibitors, inhibiting microtubule polymerization and blocking cell proliferation at metaphase during mitosis. Many CSIs were discovered or designed and synthesized as anticancer agents in the past several years and great progress had been made. Here, we discuss the insights gained so far relevant to the mechanism of CSIs and their common pharmacophore. The recent development of CSIs with their biological activity and structure-activity relationship (SAR) are also reviewed.
Export Options
About this article
Cite this article as:
Chen Jing, Liu Tao, Dong Xiaowu and Hu Yongzhou, Recent Development and SAR Analysis of Colchicine Binding Site Inhibitors, Mini-Reviews in Medicinal Chemistry 2009; 9 (10) . https://dx.doi.org/10.2174/138955709789055234
DOI https://dx.doi.org/10.2174/138955709789055234 |
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
-
Drug Resistance: Challenges to Effective Therapy
Current Cancer Drug Targets ChemoImmunoModulation: Immune Regulation by the Antineoplastic Chemotherapeutic Agents
Current Medicinal Chemistry Epithelial Mesenchymal Transition in Cancer Progression: Prev entive Phytochemicals
Recent Patents on Anti-Cancer Drug Discovery The Role of microRNAs in the Pathogenesis and Treatment of Hematopoietic Malignancies
Current Pharmaceutical Design Chemopreventive Properties of Tolfenamic Acid: A Mechanistic Review
Current Medicinal Chemistry Ketogenic Diet and Other Dietary Intervention Strategies in the Treatment of Cancer
Current Medicinal Chemistry A Comprehensive Review on the Medicinal Importance; Biological and Therapeutic Efficacy of <i>Lagenaria siceraria</i> (Mol.) (Bottle Gourd) Standley Fruit
Current Topics in Medicinal Chemistry Immunotherapeutic Approaches in MS: Update on Pathophysiology and Emerging Agents or Strategies 2006
Endocrine, Metabolic & Immune Disorders - Drug Targets Radiosyntheses using Fluorine-18: The Art and Science of Late Stage Fluorination
Current Topics in Medicinal Chemistry Anti-Cancer Activities of Tea Epigallocatechin-3-Gallate in Breast Cancer Patients under Radiotherapy
Current Molecular Medicine Potential Health Hazards for Cumulative Exposures to Phthalates and Ionizing Radiation in High-Risk Pediatric Population
Mini-Reviews in Medicinal Chemistry Antitumor Effect of Butanoylated Heparin with Low Anticoagulant Activity on Lung Cancer Growth in Mice and Rats
Current Cancer Drug Targets Mitophagy in Carcinogenesis and Tumour Progression- A New Paradigm with Emerging Importance
Anti-Cancer Agents in Medicinal Chemistry Fibrinolysis: The Key to New Pathogenetic Mechanisms
Current Medicinal Chemistry 21-Hydroxy-6,19-epoxyprogesterone: A Promising Therapeutic Agent and a Molecular Tool for Deciphering Glucocorticoid Action
Mini-Reviews in Medicinal Chemistry The Supremacy of Synergism: A Comparison of Anticancer Activity of Rhizome Extract of Bistorta Amplexicaulis and Gallic Acid in Cancer Cell Lines and Primary Cells
Current Nutraceuticals Impact of Nutrients on the Functioning of Intestinal Goblet Cells: Health and Therapeutic Perspectives
Current Nutrition & Food Science Molecular Remodeling of the Insulin Receptor Pathway by Thiazolidinediones in Type 2 Diabetes Mellitus: A Brief Review
Protein & Peptide Letters Melatonin Differentially Modulates NF-кB Expression in Breast and Liver Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry In Vivo Transdermal Delivery of Leuprolide Using Microneedles and Iontophoresis
Current Pharmaceutical Biotechnology