Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3[beta]

The synthesis, GSK-3[beta] 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...

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Published inBioorganic & medicinal chemistry letters Vol. 21; no. 19; pp. 5948 - 5951
Main Authors Cociorva, Oana M, Li, Bei, Nomanbhoy, Tyzoon, Li, Qiang, Nakamura, Ayako, Nakamura, Kai, Nomura, Masahiro, Okada, Kyoko, Seto, Shigeki, Yumoto, Kazuhiro, Liyanage, Marek, Zhang, Melissa C, Aban, Arwin, Leen, Brandon, Szardenings, Anna Katrin, Rosenblum, Jonathan S, Kozarich, John W, Kohno, Yasushi, Shreder, Kevin R
Format Journal Article
LanguageEnglish
Published 01.10.2011
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Summary:The synthesis, GSK-3[beta] 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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ObjectType-Feature-1
ISSN:0960-894X
DOI:10.1016/j.bmcl.2011.07.073