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.
IEB authors: Libor Havlíček,
René Lenobel,
Miroslav Strnad