Syntheses of xanthone derivatives and their bioactivity investigation

  1. Beidou ZhouORCID Logo,
  2. Zhimin Weng,
  3. Yugui Tong,
  4. Zetong Ma,
  5. Rongrong Wei,
  6. Jiali Li and
  7. Zihan Yu

Submitting author affiliation: Putian University, Putian, China

Beilstein Arch. 2019, 2019148. doi:10.3762/bxiv.2019.148.v1

Published 27 Nov 2019

  • Preprint

Abstract

Seventeen 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 117 were evaluated. Compounds 1012 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 activity against Candida albicans. In particular, compound 16 exhibited strong inhibitory activity against A-549 and A549/Taxol cells. Compound 17 exhibited moderate cytotoxicity against hepatoma SMMC-7721 cells. These results demonstrated that compounds 1012, 14, and 1617 are promising leads for further structural modification.

Keywords: xanthone; antitumor activity; anti-tyrosinase; antioxidation, pancreatic lipase; antifungal activity

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When a peer-reviewed version of this preprint is available in the Beilstein Journals, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:

Zhou, B.; Weng, Z.; Tong, Y.; Ma, Z.; Wei, R.; Li, J.; Yu, Z. Beilstein Arch. 2019, 2019148. doi:10.3762/bxiv.2019.148.v1

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