Abstract: Based on the study of rhodanine derivative WL-276,some novel compounds were synthesized,and their anti-tumor effects were screened by MTT method.Compounds II_1-4 were obtained by cyclization and condensation from the certain amino acids,and then coupled respectively with hydrogen sulfide donor ADT-OH to afford compounds III_1-4,whose structures were confirmed by ¹H NMR,IR and HR MS.Furthermore,preliminary pharmacological results suggested that compounds II_1,3,4,III_1-4 had strong inhibitory effects on the proliferation of HepG2 and DU145 tumor cells.Particularly,the anti-proliferation activity of compounds III_2,4 on HepG2 and compounds III_1,2,4 on DU145 tumor cells was stronger than that of the positive control,5-fluorouracil.