2. Academic Validation
  3. 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

  • 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

Affiliation

  • 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.

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