Syntheses of xanthone derivatives and their bioactivity investigation

Seventeen substituted 1-hydroxy-3-methylxanthones were synthesized in one step. The yields ranged from 33 to 76%. Then, the antitumor, antioxidant, anti-tyrosinase, anti-pancreatic lipase, and antifungal activities of compounds 1–17 were evaluated. Compounds 10–12 and 14 inhibited tyrosinase and pancreatic lipase activity to a certain extent, respectively. Compound 16 exhibited obvious cytotoxicity against fifteen cancer cells, moderate antioxidant activity, and moderate activity against Candida albicans. In particular, compound 16 exhibited strong inhibitory activity against A-549 and A549/Taxol cells. Compound 17 exhibited moderate cytotoxicity against hepatoma SMMC-7721 cells. These results demonstrated that compounds 10–12, 14, and 16–17 are promising leads for further structural modification.