Syntheses of xanthone derivatives and their bioactivity investigation.

ABSTRACT

Sixteen 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 1-16 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 inhibitory activity against Candida albicans. In particular, compound 16 exhibited strong inhibitory activity against A-549 and A549/Taxol cells. These results demonstrated that compounds 10-12, 14, and 16 are promising leads for further structural modification.[Formula see text].