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.

摘要

一步合成十六个取代的1-羟基-3-甲基氧杂蒽。产率为33％至76％。然后，抗肿瘤，抗氧化，抗酪氨酸酶，抗胰脂肪酶，和抗真菌化合物的活性1 - 16进行了评价。化合物10 – 12和14在一定程度上分别抑制了酪氨酸酶和胰脂肪酶的活性。化合物16显示出对十五种癌细胞的明显细胞毒性，适度的抗氧化活性和对白色念珠菌的适度抑制活性。特别是化合物16对A-549和A549 / Taxol细胞具有很强的抑制活性。这些结果表明，化合物10 - 12，14，和16是有希望的进一步结构修饰引线。