Synthesis of chrysin derivatives as anti-Tumor agents and relationship of their structure-activity

Objective A series of chrysin derivates was synthesized and their anti-tumor activity was evaluated to study the structure-activity relationship of chrysin derivates.Methods To synthesize a series derivates from 5,7-dihydroxyflavone by leading some small molecules with different polarities,used the chemical methods of substitution reaction,hydrolysis,amide condensation reaction,and then evaluate for their anti-proliferative activities against human cancer cell EC109,HepG2,Hela by MTT assay.Results The anti-tumor activities of Ⅲa,Ⅲb,Ⅲc,Ⅲd,Ⅲf against EC109 were better than chrysin,and the inhibitory of Ⅲa,Ⅲc,Ⅲd,Ⅲe,Ⅲf against HepG2 increased compared with chrysin,but their anti-tumor activities against Hela had no deference.Conclusion Anti-tumor effect of chrysin derivates is positively correlated with polarity of these small molecules,and chrysin derivates with high polarity display better anti-tumor activities against EC109 and HepG2 in vitro.