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

N Ogo, S Oishi, K Matsuno, J Sawada, N Fujii…

Index: Ogo, Naohisa; Oishi, Shinya; Matsuno, Kenji; Sawada, Jun-ichi; Fujii, Nobutaka; Asai, Akira Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 14 p. 3921 - 3924

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Citation Number: 45

Abstract

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.