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

…, A Nakamura, K Nakamura, M Nomura, K Okada…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5948 - 5951

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被引用次数: 8

摘要

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.