Citation: CHEN Meijun, LI Jinhai, ZHANG Zhijia, LIAO Siyan, HUANG Yan, TAN Yin. Synthesis and Anti-tumor Evaluation of Nitrile-Containing Gambogic Acid Derivatives[J]. Chinese Journal of Applied Chemistry, ;2016, 33(8): 905-912. doi: 10.11944/j.issn.1000-0518.2016.08.150397 shu

Synthesis and Anti-tumor Evaluation of Nitrile-Containing Gambogic Acid Derivatives

1.
School of Pharmaceutical Science, Guangzhou Medical University, Guangzhou 511436, China

Corresponding author: HUANG Yan, TAN Yin,
Received Date: 10 November 2015
Available Online: 29 February 2016
Fund Project:

Seven nitrile-containing gambogic acid derivatives were synthesized from gambogic acid(GA) through introducing different alkylnitriles or arylnitriles on the C-30 carboxyl of gambogic acid. Six of them are new compounds(1~6). Their structures were identified by ¹H NMR and MS analysis. The evaluation of antitumor bioactivities in vitro on the hepatoma cells(HepG2), colon adenocarcinoma cells(RKO) and ovarian adenocarcinoma cells(OVCAR-3) were done by the methylthiazolydiphenyl-tetrazolium bromide(MTT) method. The results show that most of the synthesized compounds have strong antitumor activities. Among them, the antitumor activities of compounds 4 and 6 are more potent than that of gambogic acid.
- gambogic acid,
- cyano group,
- synthesis,
- antitumor,
- derivative
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