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.

Graphical Abstract

Keywords:

• Xanthone
• antitumor activity
• anti-tyrosinase
• antioxidation
• pancreatic lipase
• antifungal activity

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

The authors gratefully thank the Leading Project of Fujian Provincial Department of Science and Technology (Grant number 2018Y0072) for the support of this program.