Synthesis of prenylated and geranylated xanthones and their bioactivities

doi:10.5246/jcps.2020.08.053

Abstract

Abstract:

Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11% to 36%. All of the compounds were first reported. Then, the antitumor, anti-tyrosinase, anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated. Compound 9 exhibited clear antitumor activity, and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin. Compounds 1–4 and 6–7 alsoexhibited certain activity other than the antitumor activity described above. These results demonstrated that compounds 1–4, 6–7and 9 were very promising leads for further structural modification.

Key words: Xanthone, Antitumor activity, Anti-tyrosinase, Antifungal activity, Antibacterial activity

CLC Number:

R915.4

Supporting:

Beidou Zhou, Zihan Yu, Yugui Tong, Jiali Li, Baocheng Huang, Rongrong Wei, Zhimin Weng, Xin Wang, Zhipeng Ruan, Jian Lin, Caihong Xu, Jianbo Liu. Synthesis of prenylated and geranylated xanthones and their bioactivities[J]. Journal of Chinese Pharmaceutical Sciences, 2020, 29(8): 564-576.

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