Synthesis And Anticancer Activities Of Bromide 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 chrysin 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 bromide chrysin derivatives.Methods:8-Bromide (13-14),6,8-di-bromide (15-18) chrysin derivatives were prepared by the reaction of Br2/C5H5N or NBS with the corresponding compouds 8,9,11, respectively. A series of B-ring bromide chrysin derivatives were prepared from 3-bromo-4-methoxybenzaldehyde or 3,5-di-bromo-4-hydroxybenzaldehyde, respectively. 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 bromide chrysin derivatives, and the derivatives were tested for their in vitro anti-cancer activities against leucocythemia (HL-60), colorectal adenocarcinoma (HT-29) and human gastric adenocarcinoma (SGC-7901) cell lines by MTT-based assay. It appeared that these closely related molecules displayed remarkable differences in cytotoxicity.Conclusion:All bromide chrysin derivatives had stronger activity than 5-Fu against HL-60 and HT-29 tumor cells. Besides compounds 2,7,16 and 17,18, bromide chrysin derivatives had stronger activity than 5-Fu against SGC-7901 tumor cells.