This invention relates to benzamide derivatives with anti-cancer activity. This invention also relates to the preparation of these compounds and their use in preparing anti-cancer drugs. In certain aspects, this invention is embodied by the poly(ADP-ribose) polymerase (PARP) inhibitors or their metabolites represented by compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, wherein R1, R2, R3 and R4 are defined in the specification.本發明涉及具有抗癌活性的苯甲醯胺衍生物。本發明也涉及到這類化合物的製備以及這類化合物在製備治療癌症的藥物上的用途。本發明在某些方面體現為,多聚(ADP-核糖)聚合酶(PARP)抑制劑或其代謝物是由式(I)所表示的化合物,或其藥學上可接受的鹽,或其前藥,其中,R1、R2、R3和R4的定義見說明書。