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.
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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 |
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