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 |
- 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
-
Vascular Endothelial Growth Factor: Adaptive Changes in the Neuroglialvascular Unit
Current Neurovascular Research TRP Channels and Cancer: New Targets for Diagnosis and Chemotherapy
Endocrine, Metabolic & Immune Disorders - Drug Targets Drug Delivery Systems Based on Polymeric Micelles and Ultrasound: A Review
Current Pharmaceutical Design Procathepsin D as a Tumor Marker, Anti-Cancer Drug or Screening Agent
Anti-Cancer Agents in Medicinal Chemistry Computational Studies Applied to Anti-inflammatory Drug Discovery: A Review
Current Organic Chemistry Drug Delivery Systems and Combination Therapy by Using Vinca Alkaloids
Current Topics in Medicinal Chemistry Culture Supernatants from Lactobacillus plantarum Induce Necrosis on a Human Promyelocytic Leukemia Cell Line
Endocrine, Metabolic & Immune Disorders - Drug Targets The Interaction of NK Cells and Dendritic Cells in the Tumor Environment: How to Enforce NK Cell & DC Action Under Immunosuppressive Conditions?
Current Medicinal Chemistry Pharmacogenomics
Current Drug Metabolism Molecule of the Month
Current Topics in Medicinal Chemistry Membrane Disrupting Lytic Peptides for Cancer Treatments
Current Pharmaceutical Design QSAR Multi-Target in Drug Discovery: A Review
Current Computer-Aided Drug Design Application of Targeted Therapy to Malignant Gliomas and Response to Treatment
Current Signal Transduction Therapy Therapeutic Implications of Superoxide Dismutase And Its Importance in Kinase Drug Discovery
Current Topics in Medicinal Chemistry Antiproliferative Activity of microRNA-125a and its Molecular Targets
MicroRNA Recent Advances in Heterocyclic Tubulin Inhibitors Targeting the Colchicine Binding Site
Anti-Cancer Agents in Medicinal Chemistry Combination Therapies of Artemisinin and its Derivatives as a Viable Approach for Future Cancer Treatment
Current Pharmaceutical Design Nucleic Acid-Based Therapeutics for Glioblastoma
Anti-Cancer Agents in Medicinal Chemistry The Clinical Impact of Quantitative Cell-free DNA, KRAS, and BRAF Mutations on Response to Anti-EGFR Treatment in Patients with Metastatic Colorectal Cancer
Current Pharmaceutical Design HLA-G - From Fetal Tolerance to a Regulatory Molecule in Inflammatory Diseases
Current Immunology Reviews (Discontinued)