The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5

被引：95

作者：

Barsanti, Paul A. ^{[1
]}

Wang, Weibo ^{[1
]}

Ni, Zhi-Jie ^{[1
]}

Duhl, David ^{[1
]}

Brammeier, Nathan ^{[1
]}

Martin, Eric ^{[1
]}

Bussiere, Dirksen ^{[1
]}

Walter, Annette O. ^{[1
]}

机构：

[1] Novartis Inst Biomed Res, Emeryville, CA 94608 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期

关键词：

Eg5; KSP; Kinesin; SPINDLE PROTEIN KSP; POTENT;

D O I：

10.1016/j.bmcl.2009.11.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of tetrahydro-beta-carbolines were identified by HTS as inhibitors of the kinesin Eg5. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of removing potential metabolic liabilities and improving cellular potency. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：157 / 160

页数：4