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
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
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DOI：
10.1016/j.bmcl.2006.08.087
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发表时间：
2006-11-15
影响因子：
2.7
通讯作者：
Rossi, Renzo
中科院分区：
文献类型：
--
作者：
Bellina, Fabio;Cauteruccio, Silvia;Rossi, Renzo
采用NCI 60人肿瘤细胞系模型，对新型combretastatin-like 1,5-和1,2- diaryl1h -咪唑的体外抗肿瘤活性进行了评价。化合物2d和2g在10(-4)-10（-8）范围内被证明比CA-4具有更大的细胞毒性。对接实验表明，所有化合物的MG_MID Log GI（50）值与其计算出的与α - β -微管蛋白的秋水秋碱结合位点的相互作用能之间具有良好的相关性。(c) 2006 Elsevier Ltd.版权所有。
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.