Design and synthesis of Grp94 selective inhibitors based on Phe199 induced fit mechanism and their anti-inflammatory effects was written by Xu, Shicheng;Guo, Anping;Chen, Nan-nan;Dai, Wei;Yang, Huan-aoyu;Xie, Wenqin;Wang, Mengjie;You, Qi-Dong;Xu, Xiao-Li. 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:
Glucose-regulated protein 94 (Grp94), a member of the Heat shock protein 90 (Hsp90) family, is implicated in many human diseases, including cancer, neurodegeneration, inflammatory, and infectious diseases. Here, we describe our effort to design and develop a new series of Grp94 inhibitors based on Phe199 induced fit mechanism. Using an alkynyl-containing inhibitor as a starting point, we developed compound 4 (I), which showed potent inhibitory activity toward Grp94 in a fluorescence polarization-based assay. With improved physicochem. properties and suitable pharmacokinetic properties, compound 4 was advanced into in vivo bioactivity evaluation. In a dextran sulfate sodium (DSS)-induced mouse model of ulcerative colitis (UC), compound 4 showed anti-inflammatory property and reduced the levels of pro-inflammatory cytokines (TNF-α and IL-6). Together, these findings provide evidence that this approach may be promising for further Grp94 drug development efforts. 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. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Liquid esters of low volatility serve as softening agents for resins and plastics. Esters also include many industrially important polymers. Polymethyl methacrylate is a glass substitute sold under the names Lucite and Plexiglas; polyethylene terephthalate is used as a film (Mylar) and as textile fibres sold as Terylene, Fortrel, and Dacron.Safety of 2-Methoxyethylamine
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem