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Design, Synthesis and Anticancer Evaluation of Fangchinoline Derivatives

1,2,†, 1,2,†, 1,2, 1,2, 1,2, 1,2, 1,2, 1,2, 1,* and 1,2,*
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, 3491 Baijin Road, Guiyang 550014, China
The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, 3491 Baijin Road, Guiyang 550014, China
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2017, 22(11), 1923;
Received: 29 September 2017 / Revised: 1 November 2017 / Accepted: 5 November 2017 / Published: 8 November 2017
PDF [1350 KB, uploaded 8 November 2017]


Twenty fangchinoline derivatives were synthesized from the natural product fangchinoline, and their anticancer activities on human breast cancer MDA-MB-231 cell line, human prostate cancer PC3 cell line, human melanoma WM9 cell line and human leukaemia HEL and K562 cell lines were evaluated. The biological result showed that those derivatives exhibited potent activities on inhibiting cancer cell growth, and the structure-activity relationships were investigated. Among them, compound 4g, which was protected by benzoyl group in 7-phenolic position and nitrified in 14-position, showed impressive inhibition on all 5 cancer cell lines, especially WM9 cell line, with an IC50 value of 1.07 µM. Further mechanistic studies demonstrated that compound 4g may induce cancer cell death by apoptotic means. These research results suggested that compound 4g could be a lead for the further development toward an anticancer agent against human melanoma WM9 in the future. View Full-Text
Keywords: fangchinoline; derivatives; anticancer activity; apoptosis fangchinoline; derivatives; anticancer activity; apoptosis

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Liu, Y.; Xia, B.; Lan, J.; Hu, S.; Huang, L.; Chen, C.; Zeng, X.; Lou, H.; Lin, C.; Pan, W. Design, Synthesis and Anticancer Evaluation of Fangchinoline Derivatives. Molecules 2017, 22, 1923.

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