6236-97-1

Usage

InChI:InChI=1/C15H13NO/c1-9-7-8-12-14(10(9)2)16-13-6-4-3-5-11(13)15(12)17/h3-8H,1-2H3,(H,16,17)

Upstream product

• 87-59-2 2,3-Dimethylaniline 
• 88-65-3 2-bromobenzoic-acid 
• 61-68-7 mefenamic Acid 
• 129833-31-4 3,4-dimethyl-2-iodobenzoic acid 
• 62-53-3 aniline 

Relevant academic research and scientific papers

Acid-catalyzed oxidative cross-coupling of acridans with silyl diazoenolates and a Rh-catalyzed rearrangement: two-step synthesis of γ-(9-acridanylidene)-β-keto esters

A MsOH-catalyzed oxidative cross-coupling of acridans and silyl diazoenolates and a Rh2(OAc)4-catalyzed rearrangement of the resultant diazo products are described. The reactions provide various γ-(9-acridanylidene)-β-keto esters in good yields, which bear an active α-methylene unit for further functionalization.

Acridone compound and medical application

The invention discloses an acridone compound and medical application. The present invention relates to compounds represented by a formula I and a formula II, racemates or optical isomers thereof, pharmaceutically acceptable salts, solvates or hydrates thereof, and uses of the compounds in preparation of STING-related antiviral or malignant tumor drugs.

Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonists

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.