Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416

被引:51
作者
Pandit, Bulbul
Sun, Yanjun
Chen, Ping
Sackett, Dan L.
Hu, Zhigen
Rich, Wendy
Li, Chenglong
Lewis, Andrew
Schaefer, Kevin
Li, Pui-KaI [1 ]
机构
[1] Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA
[2] NICHHD, Lab Integrat & Med Biophys, NIH, Bethesda, MD 20892 USA
关键词
combretastatins; SU5416; antimicrotubule; antitumor agents; cell cycle arrest; colchicine;
D O I
10.1016/j.bmc.2006.06.017
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of combretastatin A-4 analogs derived from the ATP competitive, VEGF receptor tyrosine kinase inhibitor, SU5416 were synthesized. The cytotoxic effects of the analogs were evaluated against PC-3 and MDA-MB-231 cancer cell lines, as well as their abilities to inhibit tubulin polymerization. Results are compared to those of compound 1, our lead compound previously reported. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6492 / 6501
页数:10
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