Cytochrome P450s were related to various tumorigenesis for its function as catalysts in the metabolism of endogenous and exogenous compounds.Cytochrome P450 1A1(CYP1A1) is closely related to the metabolic activation of various procarcinogens and premutagens,as well as the development of tumor.Cytochrome P450 1B1(CYP1B1) is regarded to be abnormally expressed in various human cancer cells,and participate in the oxidative metabolism of drugs and activation of prodrugs.CYP1A1 and CYP1B1 have become new targets for the study on target-oriented antitumor prodrug.Therefore,a lot of relevant researches on target-oriented antitumor pro-drugs have been reported successively.In this review,the development of target-oriented antitumor prodrugs activated by CYP1A1 and CYP1B1 are summarized according to their structures.