Synthesis and antitumor activity evaluation of chrysin derivatives

• DOI: 10.1016/j.ejmech.2013.12.044
• Publication Date: 2014-01-08T10:00:58Z
• Authors: Zhen-Yuan Zhu; Wan-Xiao Wang; Zhen-qian Wang; Li-Jing Chen; Jing-Yi Zhang; Xiao-cui Liu; Shao-ping Wu; Yong-min Zhang
• Keywords: Chrysin; IC50

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.