Identification of Simple Compounds with Microtubule-Binding Activity That Inhibit Cancer Cell Growth with High Potency

被引：65

作者：

Yang, Wan Seok ^{[1
]}

Shimada, Kenichi ^{[1
]}

Delva, Darnelle ^{[1
]}

Patel, Milesh ^{[1
]}

Ode, Egberamwen ^{[1
]}

Skouta, Rachid ^{[2
]}

Stockwell, Brent R. ^{[1
,2
,3
]}

机构：

[1] Columbia Univ, Dept Biol Sci, New York, NY 10027 USA

[2] Columbia Univ, Dept Chem, New York, NY 10027 USA

[3] Columbia Univ, Howard Hughes Med Inst, New York, NY 10027 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 01期

基金：

美国国家卫生研究院;

关键词：

Small molecules; cell-based screening; microtubule; anticancer drug leads; MULTIDRUG-RESISTANCE; TUMOR-CELLS; IN-VITRO; AGENTS; APOPTOSIS; DEATH;

D O I：

10.1021/ml200195s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We analyzed more than 1 million small molecules with the goal of finding simple synthetic compounds that potently inhibit cancer cell growth. We identified three such compounds with unknown mechanisms of action. Subsequent studies revealed that all three of these small molecules target microtubules. These three scaffolds can serve as templates for developing new microtubule-targeted agents, overcoming the limits of existing microtubule-inhibiting drugs derived from complex natural products.

引用

页码：35 / 38

页数：4

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