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Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase: synthesis, structure-activity relationship studies and antiviral activity MEDCHEMCOMM Li, J., Kovackova, S., Pu, S., Rozenski, J., De Jonghe, S., Einav, S., Herdewijn, P. 2015; 6 (9): 1666-1672

Abstract

Isothiazolo[4,3-b]pyridines are known to be endowed with potent affinity for cyclin G associated kinase (GAK). In this paper, we expanded the structure-activity relationship study by broadening the structural variety at position 3 of the isothiazolo[4,3-b]pyridine scaffold. The most potent GAK ligands (displaying Kd values of less than 100 nM) within this series carry an alkoxy group at position 3 of the central scaffold. Unfortunately, these ligands display only modest antiviral activity against the hepatitis C virus.

View details for DOI 10.1039/c5md00229j

View details for Web of Science ID 000360639300011

View details for PubMedCentralID PMC4763718