Cyclocondensation of cyanoacetamide, cyanothioacetamide and 3-aminopyrazols with sodium salt of 3-hydroxy-1-(2-naphthyl) prop-2-en-1-one gives pyridin-2-one, pyridin-2 (1H)- thione, and pyrazolo [1, 5-a] pyrimidine derivatives. These derivatives showed potent anti- tumor cytotoxic activity in vitro using different human cancer cell lines.