5042-03-5Relevant articles and documents
Combined Omics Approach Identifies Gambogic Acid and Related Xanthones as Covalent Inhibitors of the Serine Palmitoyltransferase Complex
Abegg, Daniel,Adibekian, Alexander,Dwyer, Brendan G.,Hannich, J. Thomas,Hoch, Dominic G.,Pechalrieu, Dany,Riezman, Howard,Shuster, Anton,Wang, Chao,You, Qidong,Zhang, Xiaojin
, p. 586 - 597 (2020/05/19)
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GARCINIA DERIVATIVE, ITS PREPARING METHOD AND MEDICINAL USE
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, (2012/03/26)
The present invention relates to a field of pharmaceutical chemistry, more specifically, the present invention relates to a garcinia derivative Formula (I), its preparing method, and medicinal use. Wherein the definitions of R1 and R2 are disclosed in the specification of the present invention, and the derivative of the present invention is a structurally simplified analogue of the gambogic acid compound; wherein the gambogic acid compound possesses anti-cancer characteristics, and could be used for preparation of anti-tumor drugs.
Studies on chemical modification and biology of a natural product, gambogic acid (III): Determination of the essential pharmacophore for biological activity
Wang, Xiaojian,Lu, Na,Yang, Qian,Gong, Dandan,Lin, Changjun,Zhang, Shenglie,Xi, Meiyang,Gao, Yuan,Wei, Libing,Guo, Qinglong,You, Qidong
, p. 1280 - 1290 (2011/04/22)
Caged 4-oxa-tricyclo[4.3.1.03,7]dec-2-one structural motifs are found in Garcinia natural products that demonstrate anti-tumor activity. Gambogic acid (GA, 1), the most abundant caged Garcinia xanthones, has been reported to be a promising anti-cancer agent. To identify the essential pharmacophore for its anti-tumor activity, a series of GA analogues that address potential key structural features for biological activity were synthesized, among which compound 11a displayed comparable in vitro anti-tumor activity as GA. Mechanistic studies on 11a determined that the compound induces apoptosis as well as arrests the G2/M phase of the cell cycle in HepG2 cells. The determination of the essential part of the scaffold found in GA to maintain anti-tumor effects, and the SAR based on the caged pharmacophore are reported and will provide key information for future anti-cancer drug development studies.