title: Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.
abstract: Two series of 3,4-disubstituted pyrazole analogues, 3-(benzimidazol-2-yl)-4-[2-(pyridin-3-yl)-vinyl]-pyrazoles (2) and 3-(imidazol-2-yl)-4-[2-(pyridin-3-yl)-vinyl]-pyrazoles (3), were synthesized as novel cyclin-dependent kinase (CDK) inhibitors. Representative compounds showed potent and selective CDK inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. The design, synthesis, and preliminary biological evaluation of these pyrazole compounds are reported.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development L.L.C., 1000 Route 202, Raritan, NJ 08869, USA. RLin@prdus.jnj.com
authors.forename: Ronghui
authors.initials: R
authors.lastname: Lin
authors.forename: George
authors.initials: G
authors.lastname: Chiu
authors.forename: Yang
authors.initials: Y
authors.lastname: Yu
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: Shengjian
authors.initials: S
authors.lastname: Li
authors.forename: Yanhua
authors.initials: Y
authors.lastname: Lu
authors.forename: Mary
authors.initials: M
authors.lastname: Adams
authors.forename: Angel R
authors.initials: AR
authors.lastname: Fuentes-Pesquera
authors.forename: Stuart L
authors.initials: SL
authors.lastname: Emanuel
authors.forename: Lee M
authors.initials: LM
authors.lastname: Greenberger
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011720:Pyrazoles; D018844:Cyclin-Dependent Kinases