Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase: synthesis, structure-activity relationship studies and antiviral activityElectronic supplementary information (ESI) available. See DOI: 10.1039/c5md00229j

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 K d 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. Starting from a known isothiazolo[4,3- b ]pyridine scaffold, different series of novel, potent GAK ligands were synthesized.