Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists was written by Xi, Qiumu;Wang, Mingjin;Jia, Wenqiang;Yang, Mingjian;Hu, Jinping;Jin, Jing;Chen, Xiaoguang;Yin, Dali;Wang, Xiaojian. And the article was included in Journal of Medicinal Chemistry in 2020.Product Details of 59237-53-5 This article mentions the following:
Stimulator of interferon genes (STING) is an endoplasmic reticulum-localized adaptor protein (STING receptor) that has been shown to be activated by binding to natural cyclic dinucleotide (CDN) ligands and plays a vital role in innate immune sensing of exogenous or endogenous DNA, which then induces type I interferons and other cytokines. In this paper, we described a series of amidobenzimidazole STING agonists with high potency for the STING receptor and presented the relevant structure-activity relationships (SARs). The relative potencies of compounds I, II, and III were measured by a STING competition binding assay. A more thorough study of the effect on the STING signaling pathway demonstrated that three compounds, I, II, and III, significantly increased the protein levels and mRNA levels of IFN-尾, CXCL10, and IL-6, and II as a representative compound effectively triggered the phosphorylation of STING, TBK1, and IRF3 in both human peripheral blood mononuclear cells (hPBMCs) and WT THP-1 cells. In addition, compound II demonstrated impressive antitumor efficacy in mice with established syngeneic colon tumors by i.v. administration. Furthermore, the pharmacokinetic profile of compound II was fully evaluated. In the experiment, the researchers used many compounds, for example, Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5Product Details of 59237-53-5).
Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Product Details of 59237-53-5
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics