117570-53-3Relevant articles and documents
Synthesis method of 5, 6-dimethyl xanthone-4-acetic acid
-
, (2020/09/23)
The invention relates to a preparation method of 5, 6-dichlorophenol. The invention discloses a synthetic method of 2, 6-dimethyl xanthone-4-acetic acid. According to the method, 4-chloro-5, 6-dimethyl xanthone is generated through a reaction of 2, 3-dimethylphenol and 2, 3-dichlorobenzaldehyde, then 5, 6-dimethyl xanthone-4-ethyl acetate is obtained through a reaction of 4-chloro-5, 6-dimethyl xanthone and diethyl malonate, finally, 5, 6-dimethyl xanthone-4-acetic acid is obtained through alkaline hydrolysis, the needed raw materials are moderate in price and high in yield, and the obtained product purity is higher than 98%.
Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonists
Chang, Jia-jia,Hou, Shi,Lan, Xiu-juan,Li, Song,Li, Wei,Sun, Wei,Xiao, Jun-hai,Yan, Xin-lin,Yang, Xiao-hong
, (2020/01/09)
STING (Stimulator of Interferon Genes) has become a focal point in immunology research and a target in drug discovery. The discovery of a potent human-STING agonist is expected to revolutionize current anti-virus or cancer immunotherapy. Inspired by the structure and function of murine STING-specific agonists (DMXAA and CMA), we rationally designed and synthesized four series of novel compounds for the enhancement of human sensitivity. In the cell-based assay, we identified six compounds from all the synthetic small molecules: 2g, 9g, and 12b are STING agonists that are efficacious across species, and all have the skeleton of acridone; 1b, 1c, and 12c just function in the murine STING pathway. Notably, 12b exhibits the best activity among the six agonists, and its inductions of both human and murine STING-dependent signalling are similar to that of 2′3′-cGAMP, which is a well-known STING inducer. While a protein assay indicated that 2 g, 9 g, and 12b could activate the pathway by directly binding human STING, 12b also displayed the strongest binding affinity. Additionally, our studies show that 12b can induce faster, more powerful, and more durable responses of assorted cytokines in a native system than 2′3′-cGAMP. Consequently, our team is the first to successfully modify murine STING agonists to obtain human sensitivity, and these results suggest that 12b is a potent direct-human-STING agonist. Additionally, the acridone analogues demonstrate tremendous potential in the treatment of tumours or viral infections.
5,6-DIMETHYL XANTHONE-4-ACETIC ACID DERIVATIVES AND METHOD OF PREPARING THE SAME
-
, (2010/05/13)
A method of preparation of 5,6-dimethylxanthone-4-acetic acid (DMXAA) and derivatives thereof. The derivatives are represented by formula (I), wherein R represents totally 1 to 2 substitutes at 1, 2, 3, 7, and 8 position selected from a lower alkyl, halogen, CF3, CN, NO2, NH2, CH2COOH, OR2, OH, NHSO2R2, SR2, CH2CONHR2 or NHR2, and R2 represents a lower alkyl, or a lower alkyl having OH, NH2, or OCH3. The invention further provides a pharmaceutical composition having such derivatives used as excellent antitumor and antibacterial agents.