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Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors
Authors:Lin Ronghui  Chiu George  Yu Yang  Connolly Peter J  Li Shengjian  Lu Yanhua  Adams Mary  Fuentes-Pesquera Angel R  Emanuel Stuart L  Greenberger Lee M
Institution:Johnson & Johnson Pharmaceutical Research & Development L.L.C., 1000 Route 202, Raritan, NJ 08869, USA. RLin@prdus.jnj.com
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.
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