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Bioorg Med Chem Lett. 2011 Oct 1;21(19):5948-51. doi: 10.1016/j.bmcl.2011.07.073. Epub 2011 Aug 5.

Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3β.

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


The synthesis, GSK-3β inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this class were potent and highly selective GSK-3 inhibitors.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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