3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.
A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa, HCT116, and A375 tumor cells.
Lin
Ronghui
R
Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, 1000 Route 202, Raritan, New Jersey 08869, USA. rlin@prdus.jnj.com
Lu
Yanhua
Y
Wetter
Steven K
SK
Connolly
Peter J
PJ
Turchi
Ignatius J
IJ
Murray
William V
WV
Emanuel
Stuart L
SL
Gruninger
Robert H
RH
Fuentes-Pesquera
Angel R
AR
Adams
Mary
M
Pandey
Niranjan
N
Moreno-Mazza
Sandra
S
Middleton
Steven A
SA
Jolliffe
Linda K
LK
D000631:Aminopyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D000631:Aminopyridines; D000970:Antineoplastic Agents; D003959:Diamines; D004791:Enzyme Inhibitors; D018844:Cyclin-Dependent Kinases