Document Report Card

ID: ALA3751736

Journal: Medchemcomm

Title: Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase : synthesis, structure-activity relationship studies and antiviral activity.

Authors: Li J, Kovackova S, Pu S, Rozenski J, De Jonghe S, Einav S, Herdewijn P.

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.

CiteXplore: 26925208

DOI: 10.1039/c5md00229j