Jiang, Jian-kang’s team published research in Bioorganic & Medicinal Chemistry Letters in 28 | CAS: 1416437-27-8

Bioorganic & Medicinal Chemistry Letters published new progress about 1416437-27-8. 1416437-27-8 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronate Esters,Boronic acid and ester, name is 6-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazolo[1,5-a]pyrimidine, and the molecular formula is C12H16BN3O2, Synthetic Route of 1416437-27-8.

Jiang, Jian-kang published the artcileDiscovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors, Synthetic Route of 1416437-27-8, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(20), 3356-3362, database is CAplus and MEDLINE.

The pyrazolo[1,5-a]pyrimidine LDN-193189 is a potent inhibitor of activin receptor-like kinase 2 (ALK2) but is nonselective for highly homologous ALK3 and shows only modest kinome selectivity. Herein, we describe the discovery of a novel series of potent and selective ALK2 inhibitors by replacing the quinolinyl with a 4-(sulfamoyl)naphthyl, yielding ALK2 inhibitors that exhibit not only excellent discrimination vs. ALK3 but also high kinome selectivity. In addition, the optimized compound 23 demonstrates good ADME and in vivo pharmacokinetic properties.

Bioorganic & Medicinal Chemistry Letters published new progress about 1416437-27-8. 1416437-27-8 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronate Esters,Boronic acid and ester, name is 6-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazolo[1,5-a]pyrimidine, and the molecular formula is C12H16BN3O2, Synthetic Route of 1416437-27-8.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics