Systematic structure modification of the side train of the lead compound saprothoquinone provides a series of salvicine analogues,fifteen of them were first reported.Some compounds were demonstrated potent cytotoxicity against tumor cells with the 50%inhibition concentration in the micromolar range.Furthermore some compounds showed potent topoisomeraseⅡinhibitory effects.The preliminary structure-activity relationship of saprorthoquinone analogues was discussed according to their cytotoxicity against three tumor cells. Systematic structure modification of the side train of the lead compound saprothoquinone provide a series of salvicine analogues, fifteen of them were first reported. potent topoisomeraseⅡhibitory effects.The preliminary structure-activity relationship of saprorthoquinone analogues was discussed according to their cytotoxicity against three tumor cells.