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.