Authors
Bei Li, Oana M Cociorva, Tyzoon Nomanbhoy, Qiang Li, Kai Nakamura, Masahiro Nomura, Kyoko Okada, Kazuhiro Yumoto, Marek Liyanage, Melissa C Zhang, Arwin Aban, Anna Katrin Szardenings, John W Kozarich, Yasushi Kohno, Kevin R Shreder
Publication date
2012/1/15
Journal
Bioorganic & medicinal chemistry letters
Volume
22
Issue
2
Pages
1005-1008
Publisher
Pergamon
Description
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.
Total citations
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