ABSTRACT A library of 4H-pyrido-[1,2]-pyrimidine derivatives were synthesised via one pot three component method, in this reaction involves a simple condensation of 2-minopyrimidines, aldehydes and ketones in the prescence of ethanol reflux by using cost effective and ecofriendly catalyst sulphamic acid. These synthesised compounds were submitted for the anti proliferative activity aganist various human cancer cell lines, among these 2, 3, 8 and 12 compounds were showed excellent activity. Range between 1.15- 1.95 μM.