Synthesis And Antitumor Activity Of Novel Thioacetamide Trans-stilbene Derivatives

As diet and life style changes,cancer was in high rates around the world.But there is not yet an effective way to prevent cancer,so the treatment of cancer is particularly important therefore,it is better to discover and cure cancer as soon as possible.Among cancer drugs,for its unique therapeutic mechanism and significant effect,stilbene has been widely accepted and recognized.In recent years,the important way to cure cancer is to make resveratrol as a representative of stilbene compoundsOn the basis of literatures,a novel synthetic method for stilbene derivatives via[5+1]annulation was developed,in which diketene was employed as the starting materials,which diketene was employed as the staring materials,producing 30 compounds,in which 20 intermediated products were synthesized firstly and 10 trans-stilbene derivatives.The reaction of sythesis includes four consecutive reactions:step one,preparation of substituted acetyl acetamide,step two,condensation with carbon disulfide followed by alkylation with iodomethane,step three,condensation with substituted cinnamaldehyde and step four[5+1]annulation with nitroethane.All of the synthesized acetyl amine derivative intermediates,thioacetylamine derivative intermediates and thioacetamide trans-stilbene derivatives were analyzed by LC-MAS,1H NMR and 13C NMR.The cytotoxicity of the 10 trans-stilbene derivatives was tested by MTT assay.The results indicate that compounds 5ea and 5eb both exert cytotoxic effects against human prostatic cell line PC-3(IC50=9.39?M?27.77 ?M),human hepatoma cell line HepG-2(IC50=24.39?M?32.22?M),human cancer cell line MCF-7(IC50=30.96?m 43.07?M)three tested carcinoma cell lines with better than that of resveratrol,which provides a basic science research for development of antitumor medicines.