Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
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.
Ogo
Naohisa
N
Center for Drug Discovery, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka 422-8526, Japan.
Oishi
Shinya
S
Matsuno
Kenji
K
Sawada
Jun-ichi
J
Fujii
Nobutaka
N
Asai
Akira
A
D003545:Cysteine / Q000737:chemistry* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D016547:Kinesins / Q000037:antagonists & inhibitors*
C470243:KIF11 protein, human; D016547:Kinesins; D003545:Cysteine