31271-07-5Relevant articles and documents
Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors
Jiang, Kaixuan,Gao, Biao,Yu, Jing,Jiang, Lulu,Niu, Ao,Jia, Yihe,Meng, Tao,Zhou, Lu,Wang, Jinxin
, (2021)
Phosphoglycerate mutase 1 (PGAM1) is a promising target for cancer treatment. Herein, we found that α-mangostin and γ-mangostin exhibited moderate PGAM1 inhibitory activities, with IC50 of 7.2 μM and 1.2 μM, respectively. Based on α-mangostin, a series of 1,3,6,7-tetrahydroxyxanthone derivatives were designed, synthesized and evaluated in vitro for PGAM1 inhibition. The significant structure–activity relationships (SAR) and a fresh binding mode of this kind of new compounds were also clearly described. This study provides valuable information for further optimization of PGAM1 inhibitors with 1,3,6,7-tetrahydroxyxanthone backbone or de novo design of novel inhibitor.
A preparing method and uses of mangostin and mangostin analogues
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, (2017/04/22)
The invention belongs to the fields of innovative medicines and cosmetics and particularly relates to a preparing method and uses of mangostin shown as a formula (I) and mangostin analogues shown as a formula (II). Alpha-mangostin, beta-mangostin, gamma-mangostin and analogues thereof are respectively prepared through olefination and through controlling conditions for deprotection. According to the method, products are high in purity, operation is simple and convenient, yields are high, costs are low and the method is suitable for large-scale production. On one hand, the beta-mangostin, the gamma-mangostin, beta-methoxy-mangostin, and analogues thereof have ultraviolet absorption ability and ultraviolet light radiation preventing functions so that the beta-mangostin, the gamma-mangostin, the beta-methoxy-mangostin, and the analogues thereof can be adopted as a sun-screening agent separately or compounded with other sun-screening agents and applied into cosmetics; and on the other hand, the beta-mangostin, the gamma-mangostin, the beta-methoxy-mangostin, and the analogues thereof have activity of inhibiting acid sphingomyelinase so that the beta-mangostin, the gamma-mangostin, the beta-methoxy-mangostin, and the analogues thereof can be adopted as acid sphingomyelinase inhibitors and applied for preparation of medicines for preventing and treating acid sphingomyelinase related diseases mainly including cardio cerebrovascular diseases, neurological diseases, liver diseases, lung diseases, autoimmune diseases, infectious diseases and the like.
Novel Xanthone Derivatives and Composition for Treating Cancer Comprising the Same as Active Ingredient
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Paragraph 0103; 0104; 0146; 0147, (2016/10/08)
The present invention relates to a novel xanthone derivative compound, and an anticancer composition comprising the compound as an active ingredient. The xanthone derivative compound of the present invention exhibits excellent anticancer activities against various human cancer cells and remarkably enhanced water solubility compared to an alpha-mangostin compound which is a parent compound. Therefore, the xanthone derivative compound of the present invention can be developed into anticancer drugs having excellent activities.COPYRIGHT KIPO 2016