Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 28, Issue 1, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2019.115188
Keywords
Cyclin G-associated kinase; Isothiazolo[4,3-b]pyridine; Dengue virus; Kinase inhibitor; Antiviral drugs
Funding
- Department of Defense (DoD), Congressionally Directed Medical Research Programs (CDMRP) [W81XWH-16-1-0691]
- Defense Threat Reduction Agency (DTRA), Fundamental Research to Counter Weapons of Mass Destruction [12393481]
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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-di-methoxyphenyl residue at position 5 that displayed low nanomolar GAK binding affinity and antiviral activity against dengue virus.
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