Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs

被引：30
|
作者：
Cifuentes, M
Schilling, B
Ravindra, R
Winter, J
Janik, ME [1 ]
机构：
[1] SUNY Coll Fredonia, Dept Chem, Fredonia, NY 14063 USA
[2] SUNY Binghamton, Dept Chem, Binghamton, NY 13902 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期
关键词：
colchicine; SAR; tubulin; isocolchicine; antimitotic;
D O I：
10.1016/j.bmcl.2006.02.010
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of modified colchicine and isocolchicine analogs (C-7 substituent) were synthesized and evaluated in vitro against a PC3 cancer cell line and for inhibition of microtubule polymerization. The colchicine analogs all displayed strong inhibition of tubulin polymerization, while Compounds 6 and 20 also possessed an increased cytotoxic activity as compared to colchicine. More importantly, isocolchicine analogs 7, 15, and 17 showed inhibition of microtubule polymerization with IC50 values ranging from 58 to 68 mu M. In addition, 7 displayed strong cytotoxic activity with an IC50=93 nM which was more potent than colchicine analog 12. (C) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2761 / 2764
页数：4
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