0172393 - UEB-Q 20033101 RIV NL eng J - Journal Article
Moravec, Jiří - Kryštof, Vladimír - Hanuš, Jan - Havlíček, Libor - Moravcová, Daniela - Fuksová, K. - Kuzma, Marek - Lenobel, René - Otyepka, M. - Strnad, Miroslav
2,6,8,9-Tetrasubstituted Purines as New CDK1 Inhibitors.
Bioorganic and Medicinal Chemistry Letters. Roč. 13, č. 18 (2003), s. 2993ů2996. ISSN 0960-894X. E-ISSN 1464-3405
R&D Projects: GA ČR GA301/02/0475; GA AV ČR KJB6137301
Institutional research plan: CEZ:AV0Z5020903; CEZ:AV0Z5038910
Keywords : Purine inhibitors * cyclin-dependent kinases * roscovitine
Subject RIV: EB - Genetics ; Molecular Biology
Impact factor: 2.182, year: 2003

Purine inhibitors of cyclin-dependent kinases attract attention as potential anticancer drugs because their first representative roscovitine recently entered clinical trials. Although well described in terms of structure-activity relationships, we still present here a novel modification of the purine scaffold influencing their inhibitory properties. The introduced C-8 substituents, however, lowered the CDK inhibitory activity of roscovitine, whereas the antiproliferative potential of several derivatives remained high.
Permanent Link: http://hdl.handle.net/11104/0069432