Novel halogenated sulfonamides inhibit the growth of multidrug resistant MCF-7/ADR cancer cells

被引:91
|
作者
Medina, JC [1 ]
Roche, D [1 ]
Shan, B [1 ]
Learned, RM [1 ]
Frankmoelle, WP [1 ]
Clark, DL [1 ]
Rosen, T [1 ]
Jaen, JC [1 ]
机构
[1] Tularik Inc, S San Francisco, CA 94080 USA
关键词
D O I
10.1016/S0960-894X(99)00276-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this report, we describe the synthesis of halogenated benzenesulfonamide compounds and their ability to inhibit the growth of HeLa, MCF-7 and MCF-7/ADR tumor cells in vitro. The multidrug resistance (MDR) phenotype of certain cells does not affect their sensitivity to these compounds. These agents belong to a family of compounds previously shown to bind irreversibly to cysteine-239 of beta-tubulin. Consistent with this mechanism of action, the cytotoxicities of these compounds appear to correlate with their ability to undergo nucleophilic aromatic substitution. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1843 / 1846
页数:4
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