Synthesis and antitumor, antityrosinase, and antioxidant activities of xanthone

Abstract

Ten substituted 1,3-dihydroxyxanthones were synthesized in one step. The yields ranged from 40 to 76%. Compounds 8–10 were first reported. Next, the compounds’ in vitro anti-proliferative activities against nine human cancer cell lines, antityrosinase, and antioxidant activities were evaluated. Compounds 1, 4, 6–7, and 9–10 exhibited enhanced cytotoxicity against certain cancer cells. Compounds 2, 8, 9, and 10 inhibited tyrosinase activity to a certain extent. In addition, compound 4 exhibited the best antioxidant activity, which was consistent with theoretical calculations. These results demonstrated that compounds 1–2, 4, and 6–10 were promising leads for further investigation.

Keywords:

• Xanthone
• synthesis
• antitumor activity
• antityrosinase
• antioxidation

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Acknowledgments

The authors gratefully thank the Project of Yunnan Provincial Department of Education (No. 2016ZZX200), the Education Scientific Research Project for Middle-Age and Young Teachers of Fujian Province (No. JA15453), the Science and Technology Planning Project of Putian City (No. 2014S02(3)), the Leading Project of Fujian Provincial Department of Science and Technology [grant number 2018Y0072] and the Scientific Research Projects of Putian University (Nos. 2,014,053 and 2,015,016) for supporting this program.