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Issue 9, 2015
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Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase: synthesis, structure–activity relationship studies and antiviral activity

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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.

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

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Publication details

The article was received on 28 May 2015, accepted on 03 Aug 2015 and first published on 07 Aug 2015


Article type: Concise Article
DOI: 10.1039/C5MD00229J
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Citation: Med. Chem. Commun., 2015,6, 1666-1672
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    Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase: synthesis, structure–activity relationship studies and antiviral activity

    J. Li, S. Kovackova, S. Pu, J. Rozenski, S. De Jonghe, S. Einav and P. Herdewijn, Med. Chem. Commun., 2015, 6, 1666
    DOI: 10.1039/C5MD00229J

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