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Synthesis and Evaluation of Gambogic Acid Derivatives as Antitumor Agents. Part III
Author(s) -
Guo XiaoKe,
Sun HaoPeng,
Shen Shen,
Sun Yuan,
Xie FanLei,
Tao Lei,
Guo QingLong,
Jiang Cheng,
You QiDong
Publication year - 2013
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201200126
Subject(s) - gambogic acid , chemistry , apoptosis , prenylation , annexin , lead compound , a549 cell , stereochemistry , inducer , cell culture , western blot , structure–activity relationship , biochemistry , combinatorial chemistry , in vitro , enzyme , biology , genetics , gene
Gambogic acid (GA) has been reported as a potent apoptosis inducer. Previously, we have reported chemical modification at C(34) and C(39) of GA, leading to some agents with improved activity. To investigate the further structureactivity relationship (SAR) and preliminary mechanism of GA activity, a series of derivatives with modified prenyl side chains of GA were synthesized and evaluated. Most of the derivatives showed potent inhibitory activities against the proliferation of HepG2 and A549 cell lines. Compound 4 was selected for further mechanistic studies due to its outstanding activity. It was established that 4 induces the apoptosis of HepG2 cells by using Annexin‐V/PI double staining and Western blot assay, thus, compound 4 can serve as a promising lead compound for the development of novel apoptosis in anticancer treatment.