Journal of Chinese Pharmaceutical Sciences ›› 2020, Vol. 29 ›› Issue (8): 564-576.DOI: 10.5246/jcps.2020.08.053

• Original articles • Previous Articles     Next Articles

Synthesis of prenylated and geranylated xanthones and their bioactivities

Beidou Zhou1*, Zihan Yu1, Yugui Tong2, Jiali Li1, Baocheng Huang1, Rongrong Wei1, Zhimin Weng1, Xin Wang1, Zhipeng Ruan1, Jian Lin1, Caihong Xu3, Jianbo Liu4   

  1. 1. School of Pharmacy and Medical Technology, Putian University; Key Laboratory of Pharmaceutical Analysis and Laboratory Medicine (Putian University), Fujian Province University, Putian 351100, China
    2. Putian Entry-exit Inspection and Quarantine Bureau, Putian 351100, China
    3. The Affiliated Hospital (Group) of Putian University, Putian 351100, China
    4. Lianhe Chemical Technology Co., Ltd., Taizhou 318020, China
  • Received:2020-01-12 Revised:2020-04-20 Online:2020-08-31 Published:2020-05-16
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  • Supported by:
    Leading Project of Fujian Provincial Department of Science and Technology (Grant No. 2018Y0072).


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 19 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 14 and 67 alsoexhibited certain activity other than the antitumor activity described above. These results demonstrated that compounds 14, 67and 9 were very promising leads for further structural modification. 

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

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