2. Academic Validation
  3. 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

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

  • J Med Chem. 2005 Jun 30;48(13):4208-11. doi: 10.1021/jm050267e.
Ronghui Lin 1,  Peter J Connolly,  Shenlin Huang,  Steven K Wetter,  Yanhua Lu,  William V Murray,  Stuart L Emanuel,  Robert H Gruninger,  Angel R Fuentes-Pesquera,  Catherine A Rugg,  Steven A Middleton,  Linda K Jolliffe
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Drug Discovery, 1000 Route 202, Raritan, New Jersey 08869, USA. rlin@prdus.jnj.com
PMID: 15974571 DOI: 10.1021/jm050267e
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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