Design, synthesis and biological studies of novel tubulin inhibitors

被引：13
|
作者：
Sun, Yanjun [1 ]
Pandit, Bulbul [1 ]
Chettiar, Somsundaram N. [1 ]
Etter, Jonathan P. [1 ]
Lewis, Andrew [1 ]
Johnsamuel, Jayasekar [1 ]
Li, Pui-Kai [1 ]
机构：
[1] Ohio State Univ, Div Med Chem & Pharmacognosy, Coll Pharm, Columbus, OH 43210 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 15期
关键词：
Anti-microtubule agents; Tubulin inhibitors; CONFORMATIONALLY RESTRICTED ANALOGS; COMBRETASTATIN A-4 PHOSPHATE; RECEPTOR TYROSINE KINASES; VASCULAR-TARGETING AGENT; A4; PHOSPHATE; SU5416; SCHEDULE; CANCER;
D O I：
10.1016/j.bmcl.2013.04.078
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which structurally resembles the potent anti-microtubule agent combretastatin A-4, inhibited tubulin polymerization and showed potent growth inhibitory activities on both prostate and breast cancer lines with IC50 values in the low nanomolar range. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4465 / 4468
页数：4
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