Synthesis and evaluation of isothiazolo[4,5-b]pyridines as cyclin G-associated kinase (GAK) inhibitors

Author:

Ivanova Yulia1ORCID,Spittaels Sander1,Gao Ling-Jie2ORCID,Schols Dominique3,Van Meervelt Luc4,Froeyen Mathy2ORCID,Dehaen Wim1ORCID,De Jonghe Steven3ORCID

Affiliation:

1. KU Leuven, Department of Chemistry, Sustainable Chemistry for Metals and Molecules, Celestijnenlaan 200F, B-3001 Leuven, Belgium

2. KU Leuven, Department of Pharmaceutical and Pharmacological Sciences, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Herestraat 49, box 1030, 3000 Leuven, Belgium

3. KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Herestraat 49, box 1043, 3000 Leuven, Belgium

4. KU Leuven, Department of Chemistry, Biomolecular Architecture, Celestijnenlaan 200F, B-3001 Leuven, Belgium

Abstract

A novel route to various substituted isothiazolo[4,5-b]pyridines was established. The compounds completely lacked GAK affinity, which was explained by in silico analysis.

Funder

Fonds Wetenschappelijk Onderzoek

U.S. Army Medical Research Acquisition Activity

Hercules Foundation

Publisher

Royal Society of Chemistry (RSC)

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