The Synthesis And Anticancer Activities Against MCF-7and HepG2of Genistein Derivatives

Objective: In order to search for the anticancer substances with high efficacy, lowtoxicity and provide a theoretical basis for the rational design of anticancercompounds, we introduced the alkane and trifluoromethyl into the structure ofgenistein, then we explore these compound’s anticancer activities andstructure-activity relationships.Methods: Condensation of resorcinol with m-trihydroxybenzene catalyzed by ZnCl2and followed by hydrolysis with HCl gas provided genistein and4′-trifluoromethylated flavone. The reaction of2with RX in the presence of K2CO3atreflux temperature gave genistein and4′-trifluoromethylated flavone derivatives. Wetested their anticancer activities against MCF-7(human breast cancer) andHepG2(human hepatocellular carcinoma) cells lines by MTT-Based Assay. We alsosummarized the general SAR(structure-activity relationship) of those compounds toMCF-7and HepG2cells.Results: We have synthesized and confirmed a series of genistein derivatives, and thederivatives were tested for their anti-cancer activities in vitro against MCF-7(humanbreast cancer) and HepG2(human hepatocellular carcinoma) cell lines by MTT-BasedAssay. It appeared that these closely related molecules displayed remarkabledifferences in the inhibition of MCF-7and HepG2cell’s proliferation.Conclusion: We got25new genistein derivatives and the result indicated thatcompounds4e and4o had strongest activities against MCF-7and HepG2tumor cells.