title: Synthesis and evaluation of gambogic acid derivatives as antitumor agents. Part III.
abstract: 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 structure-activity 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.
authors: State Key Laboratory of Natural Medicines, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China.
authors: Xiao-Ke
authors: XK
authors: Guo
authors: Hao-Peng
authors: HP
authors: Sun
authors: Shen
authors: S
authors: Shen
authors: Yuan
authors: Y
authors: Sun
authors: Fan-Lei
authors: FL
authors: Xie
authors: Lei
authors: L
authors: Tao
authors: Qing-Long
authors: QL
authors: Guo
authors: Cheng
authors: C
authors: Jiang
authors: Qi-Dong
authors: QD
authors: You
mesh_terms: D017304:Annexin A5 / Q000378:metabolism; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D056945:Hep G2 Cells; D006801:Humans; D013329:Structure-Activity Relationship; D044004:Xanthones / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D017304:Annexin A5; D000970:Antineoplastic Agents; D044004:Xanthones; C052659:gambogic acid