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
| Autor: | Stuart Emanuel, Yanhua Lu, Ronghui Lin, Shenlin Huang, Linda Jolliffe, Steven A. Middleton, Robert H. Gruninger, Peter J. Connolly, Steven K. Wetter, William V. Murray, Catherine A. Rugg, Angel R. Fuentes-Pesquera |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Administration
Oral Biological Availability Mice Nude Antineoplastic Agents Diamines Mice Structure-Activity Relationship Cyclin-dependent kinase In vivo Drug Discovery Animals Structure–activity relationship Enzyme Inhibitors Protein kinase A Cyclin-dependent kinase 1 Molecular Structure biology Kinase Chemistry Cyclin-dependent kinase 2 Triazoles Cyclin-Dependent Kinases In vitro Rats Biochemistry biology.protein Molecular Medicine |
| Zdroj: | Journal of Medicinal Chemistry. 48:4208-4211 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm050267e |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|