Synthesis of chrysin derivatives and screening of antitumor activity.

A series of aromatic or long-chain chrysin derivatives (1-10) were synthesized by esterification of chrysin and acyl chloride. The chemical structures of these compounds were determined by mass spectrum (MS), 1H NMR, and 13C NMR spectra. Though aromatic chrysin derivatives (1-9) with a rigid structure were hard to dissolve in common organic solvents, the long-chain chrysin derivative (10) with a flexible structure had better solubility, and its anticancer activity (IC50 = 14.79 μmol/L) against liver cancer cell lines was 5.4 times better than chrysin (IC50 = 74.97 μmol/L), which showed superposition of pharmacological activity.