Čeština
English2,6,8,9-Tetrasubstituted Purines as New CDK1 Inhibitors
Moravec, Jiří; Kryštof, Vladimír; Hanuš, Jan; Havlíček, Libor; Moravcová, Daniela; Fuksová, K.; Kuzma, Marek; Lenobel, René; Otyepka, M.; Strnad, Miroslav
BIOORGANIC AND MEDICAL CHEMISTRY LETTERS 13 [18]: 2993-2996, 2003
Keywords: Purine inhibitors; cyclin-dependent kinases; roscovitine
Abstract: 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.
DOI:
IEB authors: Libor Havlíček, René Lenobel, Miroslav Strnad
BIOORGANIC AND MEDICAL CHEMISTRY LETTERS 13 [18]: 2993-2996, 2003
Keywords: Purine inhibitors; cyclin-dependent kinases; roscovitine
Abstract: 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.
DOI: