Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors was written by Hou, Shaohua;Yang, Xiping;Yang, Yuejing;Tong, Yu;Chen, Quanwei;Wan, Boheng;Wei, Ran;Lu, Tao;Chen, Yadong;Hu, Qinghua. And the article was included in European Journal of Medicinal Chemistry in 2021.Safety of 2-Methoxyethylamine The following contents are mentioned in the article:
A series of novel ASK1 inhibitors, e.g., I and II with 1H-indazole scaffold were designed, synthesized and evaluated for their ASK1 kinase activity and AP1-HEK293 cell inhibitory effect. Systematic structure-activity relationship (SAR) efforts led to the discovery of promising compound II, which showed excellent in vitro ASK1 kinase activity and potent inhibitory effects on ASK1 in AP1-HEK293 cells. In a tumor necrosis factor-α (TNF-α)-induced HT-29 intestinal epithelial cell model, compound II exhibited a significantly protective effect on cell viability comparable to that of GS-4997; moreover, compound II exhibited no obvious cytotoxicity against HT-29 cells at concentrations up to 25μM. Mechanistic research demonstrated that compound II suppressed phosphorylation in the ASK1-p38/JNK signaling pathway in HT-29 cells and regulated the expression levels of apoptosis-related proteins. Altogether, these results showed that compound II may serve as a potential candidate compound for the treatment of inflammatory bowel disease (IBD). This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Safety of 2-Methoxyethylamine).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Safety of 2-Methoxyethylamine
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem