Song, Zilan published the artcileStructure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists, Application of 2,2-Dimethoxyethanamine, the main research area is amidobenzimidazole analog STING agonist SAR immunooncol.
Activation of the stimulator of interferon gene (STING) has emerged as an exciting immuno-oncol. therapeutic strategy; however, the first-generation STING agonists, cyclic dinucleotide (CDN) analogs, have suffered from many disadvantages and failed in clin. trials. Therefore, non-CDN small-mol. STING agonists are urgently needed. In view of the unique structure of the high potency of dimeric amidobenzimidazole STING agonist 5, a structural elaboration was conducted by modifying several structural hotspots of this scaffold. Triazole 40 was identified as a new potent STING activator, possessing EC50 values of 0.24 and 39.51μM for h- and m-STING, resp. This compound has a slightly better pharmacokinetic profile and is >20-fold more aqueously soluble than 5. It activated the STING signaling dramatically by directly binding and stabilizing all h-STING isoforms and m-STING. In vivo, intermittent administration of 40 (I) was found to have significant antitumor efficacy with good tolerance in two mouse tumor models.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Application of 2,2-Dimethoxyethanamine.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts