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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1005-8. doi: 10.1016/j.bmcl.2011.12.006. Epub 2011 Dec 8.

6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3β: discovery of nitrile derivatives with picomolar potency.

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  • 1ActivX Biosciences, Inc., 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA.


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.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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