Novel imidazole-based combretastatin A-4 analogues: Evaluation of their in vitro antitumor activity and molecular modeling study of their binding to the colchicine site of tubulin

被引：119
作者：
Bellina, Fabio
Cauteruccio, Silvia
Monti, Susanna
Rossi, Renzo
机构：
[1] Univ Pisa, Dipartimento Chim & Chim Ind, I-56126 Pisa, Italy
[2] CNR, IPCF, I-56124 Pisa, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 22期
关键词：
cytotoxicity; combretastatin A-4; colchicine; imidazoles; tubulin; molecular modeling; antitumor activity;
D O I：
10.1016/j.bmcl.2006.08.087
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The in vitro antitumor activity of novel combretastatin-like 1,5- and 1,2-diaryl-1H-imidazoles was evaluated against the NCI 60 human tumor cell lines panel. Compounds 2d and 2g proved to be more cytotoxic than CA-4 in tests involving their evaluation over a 10(-4)-10(-8) range. Docking experiments showed a good correlation between the MG_MID Log GI(50) values of all these compounds and their calculated interaction energies with the colchicine binding site of alpha beta-tubulin. (c) 2006 Elsevier Ltd. All rights reserved.
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页码：5757 / 5762
页数：6
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