Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors

被引：50

作者：

Ogo, Naohisa

Oishi, Shinya

Matsuno, Kenji

Sawada, Jun-ichi

Fujii, Nobutaka

Asai, Akira

机构：

[1] Univ Shizuoka, Sch Pharmaceut Sci, Ctr Drug Discovery, Shizuoka 422, Japan

[2] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 606, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期

关键词：

S-trityl-L-cysteine; mitotic kinesin; Eg5; inhibitor; anticancer;

D O I：

10.1016/j.bmcl.2007.04.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of Eg5 represents a novel approach for the treatment of cancer. Here, we report the synthesis and structure-activity relationship of S-trityl-L-cysteine (STLC) derivatives as Eg5 inhibitors. Some of these derivatives such as 4f demonstrated enhanced inhibitory activity against Eg5 and induced mitotic arrest with characteristic monoastral spindles in HeLa cells. (C) 2007 Elsevier Ltd. All rights reserved.

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页码：3921 / 3924

页数：4

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