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

被引：52

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 19期

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

页码：6492 / 6501

页数：10

共 33 条

[1] New antitubulin derivatives in the combretastatin A4 series:: synthesis and biological evaluation [J].