Bioorganic & Medicinal Chemistry Letters 2007-07-15

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

Naohisa Ogo, Shinya Oishi, Kenji Matsuno, Jun-ichi Sawada, Nobutaka Fujii, Akira Asai

Index: Bioorg. Med. Chem. Lett. 17 , 3921-4, (2007)

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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.