1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities |
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| Authors: | Lin Ronghui Connolly Peter J Huang Shenlin Wetter Steven K Lu Yanhua Murray William V Emanuel Stuart L Gruninger Robert H Fuentes-Pesquera Angel R Rugg Catherine A Middleton Steven A Jolliffe Linda K |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Drug Discovery, 1000 Route 202, Raritan, New Jersey 08869, USA. rlin@prdus.jnj.com |
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| Abstract: | A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 and CDK2 inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. Representative compound 3b demonstrated in vivo efficacy in a human melanoma A375 xenograft model in nude mice. |
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