期刊
CHINESE JOURNAL OF CHEMISTRY
卷 30, 期 5, 页码 1083-1091出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.201100693
关键词
gambogic acid; C-37 modified derivatives; anti-tumor activity; structure-activity relationship (SAR)
资金
- National Natural Science Foundation of China [90713038, 21072231, 30873157]
- National Major Science and Technology Project of China [2008ZX09401-001, 2009ZX09501-003]
Gambogic acid (GA, 1), the most prominent representative of Garcinia natural products, has been reported to be a promising anti-tumor agent. In order to further explore the structure-activity relationship of GA and discover novel GA derivatives as anti-tumor agents, 17 novel C-37 modified derivatives of GA were synthesized and evaluated for their in vitro anti-tumor activities against A549, HCT-116, BGC-823, HepG2 and MCF-7 cancer cell lines. Among them, 11 compounds were found to be more potent than GA against some cancer cell lines. Notably, compound 8 was almost 510 folds more active than GA against A549 and BGC-823 cell lines with the IC50 values of 0.12 mu mol center dot L-1 and 0.57 mu mol center dot L-1, respectively. Chemical modification at C-37 position of GA by introducing of hydrophilic amines could lead to increased activity and improved drug-like properties. These findings will enhance our understanding of the structure-activity relationship (SAR) of GA and lead to the discovery of novel GA derivatives as potential anti-tumor agents.
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