Synthesis And Anticancer Activities Against HepG2 And MGC-803 Of Salicylic Acid Ester Derivatives Of Chrysin

Objective: In order to dicover the high efficacy, minimum side effect and low toxicity of chrysin derivatives and provide a theoretical basis for the discovery of new anti-cancer drugs, a series of salicylate derivatives containing chrysin were synthesized, and then explore the preliminary anti-cancer activities.Methods: The salicylic acid ester derivatives of chrysin were synthesized by introducing substituted salicylic acid ester into the molecule of chrysin with C7 alkoxy as the linker. Anticancer activities of new chrysin derivatives were evaluated by MTT method on MGC-803(human gastric carcinoma cell line) and Hep G2(human hepatocellular carcinoma cell line).Results: Eighteen salicylic acid ester derivatives of chrysin were synthesized and the chemical structures of these compounds were confirmed by 1H NMR,MS. From the Anticancer bioassay activities results, most of the synthetic chrysin compounds displayed a moderate degree of anticancer activity in human gastric carcinoma cell line MGC-803 and human hepatocellular carcinoma cell line Hep G2. compounds 5c?6a?6c?7a?7c?8b?9a?9b exhibited the most potent inhibitory with IC50(half maximal inhibitory concentration) than positive control drug 5-Fu in human hepatocellular carcinoma cell line Hep G2. Compounds 6c?10a?10b exhibited the most potent inhibitory with IC50(half maximal inhibitory concentration) than positive control drug 5-Fu in human gastric carcinoma cell line MGC-803.Conclusion: Eighteen salicylate derivatives containing chrysin were designed and synthesized. The preliminary biological results have demonstrated that some salicylate derivatives containing chrysin derivatives exhibited the better activities than positive control drug 5-Fu, which provides a new train of thought For the further development of chrysin anticancer drugs.