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

doi:10.11944/j.issn.1000-0518.2016.08.150397

Chinese Journal of Applied Chemistry ›› 2016, Vol. 33 ›› Issue (8): 905-912.DOI: 10.11944/j.issn.1000-0518.2016.08.150397

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

CHEN Meijun,LI Jinhai,ZHANG Zhijia,LIAO Siyan,HUANG Yan(),TAN Yin()

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

Received:2015-11-10 Accepted:2016-02-29 Published:2016-07-21 Online:2016-07-21
Contact: HUANG Yan,TAN Yin
Supported by:
Supported by Science and Technology Planning Project of Guangdong Province(No.2013B031800021)

Abstract

Abstract:

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.

Key words: gambogic acid, cyano group, synthesis, antitumor, derivative

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.

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

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