Synthesis and antitumor activity evaluation of chrysin derivatives

Abstract A series of 5,7-disubstituted chrysin, 7-monosubstituted chrysin, 5-monosubstituted chrysin derivatives were synthesized by alkylation, acetylation, benzoylation, carboxymethylation, and evaluated on their antitumor activity of H22 cells in the search for potential antitumor agents. Among them, compound 3 (5,7-diacetyl chrysin) displayed the most potent antitumor activity with IC 50 value of 141 μM. Moreover, there is significant up-regulation of G2 in cell cycle of H22.