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
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 13期
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.
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收藏
页码：1843 / 1846
页数：4
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