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Synthesis of a 3,7-Disubstituted Isothiazolo[4,3- b ]pyridine as a Potential Inhibitor of Cyclin G-Associated Kinase.
- Source :
-
Molecules . Mar2024, Vol. 29 Issue 5, p954. 16p. - Publication Year :
- 2024
-
Abstract
- Disubstituted isothiazolo[4,3-b]pyridines are known inhibitors of cyclin G-associated kinase. Since 3-substituted-7-aryl-isothiazolo[4,3-b]pyridines remain elusive, a strategy was established to prepare this chemotype, starting from 2,4-dichloro-3-nitropyridine. Selective C-4 arylation using ligand-free Suzuki-Miyaura coupling and palladium-catalyzed aminocarbonylation functioned as key steps in the synthesis. The 3-N-morpholinyl-7-(3,4-dimethoxyphenyl)-isothiazolo[4,3-b]pyridine was completely devoid of GAK affinity, in contrast to its 3,5- and 3,6-disubstituted congeners. Molecular modeling was applied to rationalize its inactivity as a GAK ligand. [ABSTRACT FROM AUTHOR]
- Subjects :
- *CYCLINS
*PYRIDINE
*ARYLATION
*IMIDAZOPYRIDINES
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 29
- Issue :
- 5
- Database :
- Academic Search Index
- Journal :
- Molecules
- Publication Type :
- Academic Journal
- Accession number :
- 175992031
- Full Text :
- https://doi.org/10.3390/molecules29050954