Ogo Naohisa, Oishi Shinya, Matsuno Kenji, Sawada Jun-ichi, Fujii Nobutaka, Asai Akira
Center for Drug Discovery, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka 422-8526, Japan.
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3921-4. doi: 10.1016/j.bmcl.2007.04.101. Epub 2007 May 3.
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.
抑制驱动蛋白 Eg5 是一种治疗癌症的新方法。在此，我们报告了作为 Eg5 抑制剂的 S-三苯甲基-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，对 Eg5 表现出增强的抑制活性，并在 HeLa 细胞中诱导出具有特征性单星体纺锤体的有丝分裂停滞。
