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 - were evaluated. Compounds - and inhibited tyrosinase and pancreatic lipase activity to a certain extent, respectively. Compound exhibited obvious cytotoxicity against fifteen cancer cells, moderate antioxidant activity, and moderate inhibitory activity against . In particular, compound exhibited strong inhibitory activity against A-549 and A549/Taxol cells. These results demonstrated that compounds -, , and are promising leads for further structural modification.[Formula: see text].
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