Pryde, David C.; Middya, Sandip; Banerjee, Monali; Shrivastava, Ritesh; Basu, Sourav; Ghosh, Rajib; Yadav, Dharmendra B.; Surya, Arjun published an article in 2021. The article was titled 《The discovery of potent small molecule activators of human STING》, and you may find the article in European Journal of Medicinal Chemistry.Category: esters-buliding-blocks The information in the text is summarized as follows:
The adaptor protein STING plays a major role in innate immune sensing of cytosolic nucleic acids, by triggering a robust interferon response. Despite the importance of this protein as a potential therapeutic target for serious unmet medical conditions including cancer and infectious disease there remains a paucity of STING ligands. Starting with a benzothiazinone series of weak STING activators (human EC50 ∼10μM) we identified several chemotypes with sub-micromolar STING activity across all the major protein polymorphs. An example compound I, based on an oxindole core structure, demonstrated robust on-target functional activation of STING (human EC50 185 nM) in immortalized and primary cells and a cytokine induction fingerprint consistent with STING activation. Our study has identified several related series of potent small mol. human STING activators with potential to be developed as immunomodulatory therapeutics. The experimental part of the paper was very detailed, including the reaction process of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Category: esters-buliding-blocks)
Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Category: esters-buliding-blocksMethyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics