Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4
Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4
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DOI：
10.1016/j.bmcl.2008.07.070
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发表时间：
2008-09-15
影响因子：
2.7
通讯作者：
Pinney, Kevin G.
中科院分区：
文献类型：
--
作者：
Hall, John J.;Sriram, Madhavi;Pinney, Kevin G.
一种新的三氟氨基考布他汀类似物（Z）-2-（40-甲氧基-3 '-氨基苯基）-1-（3，4，5-三氟苯基）乙烯是一种有效的微管蛋白组装抑制剂（IC_（50）= 2.9 μ M），对某些人癌细胞系具有细胞毒性。这种新的先导化合物是一组相关结构修饰中最活跃的化合物之一。(C)2008爱思唯尔有限公司保留所有权利。
A new trifluorinated amino-combretastatin analogue, (Z)-2-(40-methoxy-3'-aminophenyl)-1-(3,4,5-trif uorophenyl) ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC50 = 2.9 mu M), and cytotoxic against selected human cancer cell lines. This new lead compound is among the most active from a group of related structural modifications. (C) 2008 Elsevier Ltd. All rights reserved.