6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3β: Discovery of nitrile derivatives with picomolar potency
Copyright policy )6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3β: Discovery of nitrile derivatives with picomolar potency
We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
- Torrey Pines Institute For Molecular Studies United States
Staphylococcus aureus, Glycogen Synthase Kinase 3 beta, Dose-Response Relationship, Drug, Molecular Structure, Stereoisomerism, Microbial Sensitivity Tests, Anti-Bacterial Agents, Glycogen Synthase Kinase 3, Structure-Activity Relationship, Nitriles, Escherichia coli, Enzyme Inhibitors, Quinolizines
Staphylococcus aureus, Glycogen Synthase Kinase 3 beta, Dose-Response Relationship, Drug, Molecular Structure, Stereoisomerism, Microbial Sensitivity Tests, Anti-Bacterial Agents, Glycogen Synthase Kinase 3, Structure-Activity Relationship, Nitriles, Escherichia coli, Enzyme Inhibitors, Quinolizines
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