《Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors》 was written by Qhobosheane, Malikotsi A.; Legoabe, Lesetja J.; Josselin, Beatrice; Bach, Stephane; Ruchaud, Sandrine; Petzer, Jacobus P.; Beteck, Richard M.. Electric Literature of C3H6O2 And the article was included in Bioorganic & Medicinal Chemistry in 2020. The article conveys some information:
The synthesis and biol. evaluation of new 7-azaindole derivatives I [X = O, CH2, (CH2)2, CH2O, CH2S; R = H, 6-OH, 6,7-(MeO)2, etc.] bearing benzocycloalkanone motifs as potential protein kinase inhibitors are reported. Four compounds I [X = (CH2)2, R = H, 6-OH; X = CH2, R = 5,6-(MeO)2; X = O, R = 6-OH] were discovered to inhibit cyclin-dependent kinase 9 (CDK9/CyclinT) and/or Haspin kinase in the micromolar to nanomolar range. The compound I [X = O, R = 6-OH] was identified as the most potent Haspin inhibitor (IC50 = 14 nM), while I [X = (CH2)2; R = H, 6-OH] acted as dual inhibitors of CDK9/CyclinT and Haspin. These novel compounds constitute a promising starting point for the discovery of dual protein kinase inhibitors that have potential to be developed as anticancer agents, since both CDK9/CyclinT and Haspin are considered to be drug targets in oncol. In the experimental materials used by the author, we found Oxetan-3-ol(cas: 7748-36-9Electric Literature of C3H6O2)
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.Electric Literature of C3H6O2
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