Recent Development and SAR Analysis of Colchicine Binding Site Inhibitors

被引：77

作者：

Chen, Jing ^{[1
]}

Liu, Tao ^{[1
]}

Dong, Xiaowu ^{[1
]}

Hu, Yongzhou ^{[1
]}

机构：

[1] Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2009年 / 9卷 / 10期

关键词：

Microtubules; colchicine binding site; inhibitor; SAR; anticancer; COMBRETASTATIN A-4 ANALOGS; CIS-RESTRICTED ANALOGS; ALPHA-BETA-TUBULIN; HUMAN CANCER-CELLS; BIOLOGICAL EVALUATION; ANTIMITOTIC AGENTS; ANTITUMOR AGENTS; IN-VIVO; ANTINEOPLASTIC AGENTS; POTENT INHIBITORS;

D O I：

10.2174/138955709789055234

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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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收藏

页码：1174 / 1190

页数：17

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