Synthesis And Anticancer Activities Of Apigenin Derivatives

Objective: Apigenin has shown antitumor activities in breast cancer, prostate cancer, colon cancer, and so on. However, the anticancer activity of apigenin is low because it is not or little absorbed in intestines. In order to search for anticancer substances with high efficacy, low toxicity and minimum side effects. We are interested in the synthesis and anticancer effect of apigenin derivatives.Methods: Using modified Baker-Venkataraman transformation, a series of apigenin derivatives were synthesized though introducing-CF3,-OCF2 H,-NO2 and-OCH3 into the different position of Apigenin B ring respectively. We tested their anticancer activities against leucocythemia(HL-60) and colorectal adenocarcinoma(HT-29) cells lines by MTT-Based Assay.Results: We have synthesized a series of apigenin derivatives, its structure was identified firstly by the use of IR, 1H-NMR, MS, EA. All the derivatives were tested for their in vitro anti-cancer activities against leucocythemia(HL-60) and colorectal adenocarcinoma(HT-29) cell lines by MTT-Based Assay. It appeared that these closely related molecules displayed remarkable differences in cytotoxicity.Conclusion: 18 apigenin derivatives including 8 new compounds were synthesized. Compound 6 had the strongest activity against HL-60 and HT-29 tumor cells, even than 5-FU.