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Articles

Synthesis and antitumor, antityrosinase, and antioxidant activities of xanthone

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Pages 467-476 | Received 30 Nov 2017, Accepted 14 Mar 2018, Published online: 30 Mar 2018
 

Abstract

Ten substituted 1,3-dihydroxyxanthones were synthesized in one step. The yields ranged from 40 to 76%. Compounds 810 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, 67, and 910 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 12, 4, and 610 were promising leads for further investigation.

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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.

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