Structure-activity Relationship of Gambogic Acid

ABSTRACTAIMTo investigate the basic structure-activity relationship of gambogic acid.METHODSThrough simplifying the complex skeleton of the natural gambogic acid, two series of derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method.RESULTSThe cytotoxic activities of all these small compounds with planar ring were much less potent than those of the natural gambogic acid, and the introduction of prenyl to these small molecular compounds could increase their antitumor activities.CONCLUSIONThe structure-activity relationship of synthesized compounds indicated that the prenyl groups and the bridge core in gambogic acid were very important for keeping its antitumor activities.