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Bioorg Med Chem Lett. 2007 Jul 15;17(14):3921-4. Epub 2007 May 3.

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

Author information

1
Center for Drug Discovery, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka 422-8526, Japan.

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.

PMID:
17524640
DOI:
10.1016/j.bmcl.2007.04.101
[Indexed for MEDLINE]

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