Design, synthesis and anticancer activity of 1-acyl-3-amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives

A series of novel 1-acyl-3-amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives was designed, synthesized and evaluated as potential anticancer agents. The activity of compound 11a (IC50: 0.58-2.13 μM) was best from 4-fold to 28-fold more than that of (R)-roscovitine against six human cancer cell lines. 11a also has promising inhibitory activities against both cyclin-dependent kinase 5/p25 (CDK5/p25) and glycogen synthase kinase-3β (GSK3β).