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 topoisomerase Ⅱ inhibitory effects. The preliminary structure-activity relationship of saprorthoquinone analogues was discussed according to their cytotoxicity against three tumor cells.