A novel series of 3, 5, 6-trisubstituted pyrazolo [4, 3-d] pyrimidin-7-one derivatives, especially 6-N-arylcarboxamidopyrazolo [4, 3-d] pyrimidin-7-ones were synthesized and evaluated for their in vitro anticancer activities against various human cancer cell lines. The inhibitory activities for several kinases have also been tested. The prepared compounds library exhibited significant anticancer activity towards HT-29 colon and DU-145 prostate ...