Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors
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DOI：
10.1016/j.bmcl.2007.04.101
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发表时间：
2007-07-15
影响因子：
2.7
通讯作者：
Asai, Akira
中科院分区：
文献类型：
--
作者：
Ogo, Naohisa;Oishi, Shinya;Asai, Akira
抑制Eg5是一种治疗癌症的新方法。本文报道了作为Eg5抑制剂的s -三酰基- l-半胱氨酸（STLC）衍生物的合成及其构效关系。其中一些衍生物，如4f，显示出对Eg5的增强抑制活性，并在HeLa细胞中诱导具有特征性单星纺锤体的有丝分裂停止。(C) 2007 Elsevier Ltd.版权所有。
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.