Objective To design and synthesize genistein mono-sulfate and investigate their effects on proliferation of MCF-7 breast cancer cells.Methods Genistein-7-sulfate was achieved by reaction of chlorosulfonic acid with genistein-4′-hexanate,which was synthesized via the reaction of genistein with hexanoyl chloride.Genistein-4′-sulfate was synthesized via the reaction of genistein with benzoyl chloride,followed by treatment with chlorosulfonic acid.Results and Conclusion The structures of target compounds were identified by 1H-NMR and MS.MTT test showed that genistein induced proliferation of MCF-7 breast cancer cells,while its sulfate inhibited the proliferation at the concentration of 4.5 mmol·L-1.