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