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Structure-activity relationship study of the pyridine moiety of isothiazolo[4, 3-b]pyridines as antiviral agents targeting cyclin G-associated kinase

Journal Contribution - Journal Article

Previously, we reported the discovery of 3,6-disubstituted isothiazolo[4,3-b]pyridines as potent and selective cyclin G-associated kinase (GAK) inhibitors with promising antiviral activity. In this manuscript, the structure-activity relationship study was expanded to synthesis of isothiazolo[4,3-b]pyridines with modifications of the pyridine moiety. This effort led to the discovery of an isothiazolo[4,3-b]pyridine derivative with a 3,4-dimethoxyphenyl residue at position 5 that displayed low nanomolar GAK binding affinity and antiviral activity against dengue virus.
Journal: Bioorganic & Medicinal Chemistry
ISSN: 0968-0896
Issue: 1
Volume: 28
Publication year:2020
BOF-keylabel:yes
IOF-keylabel:yes
BOF-publication weight:1
CSS-citation score:1
Authors:International
Authors from:Higher Education
Accessibility:Open