8-Azapurines as new inhibitors of cyclin-dependent kinases

0083397 - ÚEB 2008 RIV GB eng J - Journal Article
Havlíček, Libor - Fuksová, Květoslava - Kryštof, Vladimír - Orság, Martin - Vojtěšek, B. - Strnad, Miroslav
8-Azapurines as new inhibitors of cyclin-dependent kinases.
[8-Azapurines as new inhibitors of cyclin-dependent kinases.]
Bioorganic & Medicinal Chemistry. Roč. 13, č. 8 (2005), s. 5399-5407. ISSN 0968-0896. E-ISSN 1464-3391
R&D Projects: GA AV ČR KJB6137301; GA ČR GA301/05/0418
Institutional research plan: CEZ:AV0Z50380511
Source of funding: V - Other public resources ; V - Other public resources
Keywords : CDK2 * Inhibitor * Anticancer drug
Subject RIV: FD - Oncology ; Hematology
Impact factor: 2.286, year: 2005

Purine inhibitors of cyclin-dependent kinases (CDK) seem to be a potential anticancer drug candidate as one of the first representatives, roscovitine, is passing Phase II clinical trials for cancer and glomerulonephritis. In this article, we describe a novel modification of the purine scaffold influencing CDK2 inhibitory activities as well as anticancer properties in cell lines of different histopathological origin. The introduced N at position 8 of the purine ring generally lowered CDK2 inhibitory activity of new 8-azapurines (1,2,3-triazolo[4,5-d]pyrimidines) in comparison to the model trisubstituted purines, whereas the antiproliferative potential of some derivatives remained very high, reflecting their ability to activate p53 tumor suppressor.

8-Azapurines as new inhibitors of cyclin-dependent kinases.
Permanent Link: http://hdl.handle.net/11104/0146656