Title of article :
2,6,8,9-Tetrasubstituted Purines as New CDK1 Inhibitors
Author/Authors :
Ji ? Moravec، نويسنده , , Vladim?r Kry tof، نويسنده , , Jan Hanu ، نويسنده , , Libor Havl? ek، نويسنده , , Daniela Moravcov?، نويسنده , , Kv toslava Fuksov?، نويسنده , , Marek Kuzma، نويسنده , , René Lenobel، نويسنده , , Michal Otyepka، نويسنده , , Miroslav Strnad، نويسنده ,
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.
