title: Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase : synthesis, structure-activity relationship studies and antiviral activity.
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.
authors.affiliation: KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium ; KU Leuven, Interface Valorisation Platform, Kapucijnenvoer 33, 3000 Leuven, Belgium.
authors.forename: Jiahong
authors.initials: J
authors.lastname: Li
authors.affiliation: KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium ; KU Leuven, Interface Valorisation Platform, Kapucijnenvoer 33, 3000 Leuven, Belgium.
authors.forename: Sona
authors.initials: S
authors.lastname: Kovackova
authors.affiliation: Department of Medicine, Division of Infectious Diseases and Geographic Medicine, and Department of Microbiology and Immunology, Stanford University School of Medicine, Stanford, California, USA.
authors.forename: Szuyuan
authors.initials: S
authors.lastname: Pu
authors.affiliation: KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.
authors.forename: Jef
authors.initials: J
authors.lastname: Rozenski
authors.affiliation: KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium ; KU Leuven, Interface Valorisation Platform, Kapucijnenvoer 33, 3000 Leuven, Belgium.
authors.forename: Steven
authors.initials: S
authors.lastname: De Jonghe
authors.affiliation: Department of Medicine, Division of Infectious Diseases and Geographic Medicine, and Department of Microbiology and Immunology, Stanford University School of Medicine, Stanford, California, USA.
authors.forename: Shirit
authors.initials: S
authors.lastname: Einav
authors.affiliation: KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium ; KU Leuven, Interface Valorisation Platform, Kapucijnenvoer 33, 3000 Leuven, Belgium.
authors.forename: Piet
authors.initials: P
authors.lastname: Herdewijn