Structure-activity relationship study of the pyridine moiety of isothiazolo[4,3-b]pyridines as antiviral agents targeting cyclin G-associated kinase.

Belén Martinez-Gualda,Szu-Yuan Pu,Mathy Froeyen,Piet Herdewijn,Shirit Einav,Steven De Jonghe

Bioorganic & Medicinal Chemistry（2020）

引用 13|浏览16

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摘要

•Novel 3,5- and 3,6-disubstituted isothiazolo[4,3-b]pyridines were synthesized.•Compounds were evaluated for GAK binding affinity.•The most potent isothiazolo[4,3-b]pyridine analogue was endowed with a GAK IC50 value of 0.024 µM.•This compound also exhibited antiviral activity against dengue virus.

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关键词

Cyclin G-associated kinase,Isothiazolo[4,3-b]pyridine,Dengue virus,Kinase inhibitor,Antiviral drugs

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