《Discovery of a novel class of covalent dual inhibitors targeting the protein kinases BMX and BTK》 was written by Forster, Michael; Liang, Xiaojun Julia; Schroeder, Martin; Gerstenecker, Stefan; Chaikuad, Apirat; Knapp, Stefan; Laufer, Stefan; Gehringer, Matthias. Reference of Oxetan-3-ol And the article was included in International Journal of Molecular Sciences in 2020. The article conveys some information:
Here a novel class of dual BMX/BTK inhibitors, which were designed from irreversible inhibitors of Janus kinase (JAK) 3 targeting a cysteine located within the solvent-exposed front region of the ATP binding pocket was presented. Structure-guided design exploiting the differences in the gatekeeper residues enabled the achievement of high selectivity over JAK3 and certain other kinases harboring a sterically demanding residue at this position. The most active compounds inhibited BMX and BTK with apparent IC50 values in the single digit nanomolar range or below showing moderate selectivity within the TEC family and potent cellular target engagement. These compounds represent an important first step towards selective chem. probes for the protein kinase BMX. The experimental part of the paper was very detailed, including the reaction process of Oxetan-3-ol(cas: 7748-36-9Reference of Oxetan-3-ol)
Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Reference of Oxetan-3-ol
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