Formula: C3H6O2In 2021 ,《Synthesis, biological evaluation, and docking studies of novel pyrrolo[2,3-b]pyridine derivatives as both ectonucleotide pyrophosphatase/phosphodiesterase inhibitors and antiproliferative agents》 appeared in European Journal of Medicinal Chemistry. The author of the article were Ullah, Saif; El-Gamal, Mohammed I.; El-Gamal, Randa; Pelletier, Julie; Sevigny, Jean; Shehata, Mahmoud K.; Anbar, Hanan S.; Iqbal, Jamshed. The article conveys some information:
A series of sulfonylurea derivatives possessing pyrrolo[2,3-b]pyridine core I (R = H, 5-Br, 4-Cl, 4-NMe2; Ar = Ph, 3-O2NC6H4, 2-naphthyl, etc.) were synthesized and investigated as inhibitors of NPP1 and NPP3 isoenzymes that are over-expressed in cancer and diabetes. The enzymic evaluation highlighted compound I (R = H; Ar = Ph) as selective NPP1 inhibitor, however, compound I (R = H; Ar = 3-O2NC6H4) was observed as the most potent inhibitor of NPP1 with an IC50 value of 0.80 +/- 0.04μM. Compound I (R = 4-NMe2; Ar = Ph) was found to be the most potent and moderately selective inhibitor of NPP3 (IC50 = 0.55 +/- 0.01μM). Furthermore, in vitro cytotoxicity assays of compounds against MCF-7 and HT-29 cancer cell lines exhibited compound I (R = H; Ar = 3-O2NC6H4) (IC50 = 4.70 +/- 0.67μM), and I (R = 5-Br; Ar = 4-MeC6H4) (IC50 = 1.58 +/- 0.20μM) as the most cytotoxic compounds against MCF-7 and HT-29 cancer cell lines, resp. Both the investigated compounds showed high degree of selectivity towards cancer cells than normal cells (WI-38). Mol. docking studies of selective and potent enzyme inhibitors revealed promising mode of interactions with important binding sites residues of both isoenzymes i.e., Thr256, His380, Lys255, Asn277 residues of NPP1 and His329, Thr205, and Leu239 residues of NPP3. In addition, the most potent antiproliferative agent, compound I (R = 5-Br; Ar = 4-MeC6H4), doesn’t produce hypoglycemia as a side effect when injected to mice which is an addnl. merit of this promising compound After reading the article, we found that the author used Oxetan-3-ol(cas: 7748-36-9Formula: 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.Formula: C3H6O2
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts