Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors.
Substituted benzimidazoles were profiled as inhibitors of kinesin spindle protein (KSP), an increasingly important target for the development of anticancer drugs. This series demonstrated the monoastral phenotypic response and was found to be active in both enzymatic and cellular-based assays.
Lahue
Brian R
BR
Schering-Plough Research Institute, 320 Bent Street, Cambridge, MA 02141, USA. brian.lahue@spcorp.com
Ma
Yao
Y
Shipps
Gerald W
GW
Seghezzi
Wolfgang
W
Herbst
Ronald
R
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018938:Caco-2 Cells; D002460:Cell Line; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D016547:Kinesins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D004791:Enzyme Inhibitors; C470243:KIF11 protein, human; D003577:Cytochrome P-450 Enzyme System; C031000:benzimidazole; D016547:Kinesins