Author/Authors :
Kirk L. Stevens، نويسنده , , Michael J. Reno، نويسنده , , Jennifer B. Alberti، نويسنده , , Daniel J. Price، نويسنده , , Laurie S. Kane-Carson، نويسنده , , Victoria B. Knick، نويسنده , , Lisa M. Shewchuk، نويسنده , , Anne M. Hassell، نويسنده , , James M. Veal، نويسنده , , Stephen T. Davis، نويسنده , , Robert J. Griffin، نويسنده , , Michael R. Peel، نويسنده ,
Abstract :
A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modification of the hinge-binding amine or the C(2)- and C(6)-substitutions on the pyrazolopyridazine core provided potent inhibitors of CDK4 and demonstrated enzyme selectivity against VEGFR-2 and GSK3β.
Keywords :
cancer , Cyclin-dependant kinase inhibitor , CDK2 , Cdk4 , VEGFR-2 , GSK3? , 5-b] pyridazine
