Synthesis And Anticancer Activities Of Iodo-chrysin Derivatives

Objective:Chrysin, one kind of widely distributed flavonoids in nature, has been reported to have anticancer activity. However, the anticancer activity of chrysin was low because it was not or little absorbed in intestines. In order to search for anticancer substances with high efficacy, low toxicity and minimum side effects. We were interested in the synthesis and anticancer effect of iodo-chrysin derivatives.Methods:6-iodo, 8-iodo and 6,8-di-iodo-chrysin derivatives were prepared by the reaction of ICl and I2 with the corresponding chrysin. 3'-iodo-chrysin derivatives were synthesized from 3-iodo-4-methoxy-benzaldehyde. We tested their anticancer activities against leucocythemia (HL-60), colorectal adenocarcinoma (HT-29)and human gastric adenocarcinoma (SGC-7901) cells lines by MTT-Based Assay.Results:We have synthesized a series of iodo-chrysin derivatives , and these derivatives were tested for their in vitro anti-cancer activities against HL-60, HT-29 and SGC-7901 cell lines by MTT-Based Assay. It indicated that these closely related molecules displayed remarkable differences in cytotoxicity.Conclusion:Structure-activity relationships demonstrated that iodo-chrysin derivatives which introduced the iodine into A-ring or B-ring had stronger activity than chrysin against HL-60 tumor cells. However, the B-iodo-chrysin derivatives showed weaker activity than chrysin in rejecting HT-29 and SGC-7901 tumor cells.