Abstract: Galangin,a naturally occurring bioflavonoid,has a variety of pharmacological effects.However,few literatures on its structural modification have been reported.In the present study,five nitrogen-containing galangin derivatives were designed and synthesized,the structures of the synthesized derivatives were characterized by 1H NMR, 13C NMR and MS,then the antitumor activities of these derivatives were assayed by MTT method.The results showed that the antiproliferative activity against human prostatic carcinoma cell line PC-3 of 2-phenyl-3,5,7-trihydroxy-8-(morpholinomethyl)-4H-chromen-4-one 2c(IC50 11.37 μmol/L) and 2-phenyl-3,5,7-trihydroxy-8-(piperazin-1-ylmethyl)-4H-chromen-4-one 2d(IC50:13.57μmol/L) were more potent than galangin(IC50:41.66 μmol/L) while the compound 2d exhibited the highest anti-proliferative activity against human colon cancer cell line Lovo with about 5.22-fold more potent than galangin.The increase of the antitumor activities of these derivatives was possibly related to the introduction of N-containing heterocyclic ring into the 8-site of galangin.

Key words: galangin, structural modification, nitrogen heterocyclic compounds, antitumor activity