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

  • Bioorg Med Chem Lett. 2007 Jul 15;17(14):3921-4. doi: 10.1016/j.bmcl.2007.04.101.
Naohisa Ogo  1 ,  Shinya Oishi ,  Kenji Matsuno ,  Jun-ichi Sawada ,  Nobutaka Fujii ,  Akira Asai
Affiliations
  • 1. Center for Drug Discovery, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka 422-8526, Japan.
PMID: 17524640 DOI: 10.1016/j.bmcl.2007.04.101
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.