Synthesis and antitumor activity evaluation of chrysin derivatives

•A series of chrysin derivatives was firstly synthesized.•5,7-Diacetyl chrysin derivative displayed the most potent anti-tumor activity.•The IC50 value of 5,7-diacetyl chrysin derivative on H22 cells was 141 μM.

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 IC50 value of 141 μM. Moreover, there is significant up-regulation of G2 in cell cycle of H22.

Graphical abstractA 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.Figure optionsDownload full-size imageDownload as PowerPoint slide