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

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.

Bioorg Med Chem Lett ; 21(19): 5948-51, 2011 Oct 01.

Article in English | MEDLINE | ID: mdl-21873061

ABSTRACT

The synthesis, GSK-3ß 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.

Subject(s)

Glycogen Synthase Kinase 3/antagonists & inhibitors , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/pharmacology , 4-Quinolones/chemistry , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Clinical Trials as Topic , Drug Design , Drug Evaluation, Preclinical , Glycogen Synthase Kinase 3/metabolism , Glycogen Synthase Kinase 3 beta , HL-60 Cells , High-Throughput Screening Assays , Humans , Inhibitory Concentration 50 , Isoenzymes , Molecular Targeted Therapy , Protein Kinase Inhibitors/chemistry , Structure-Activity Relationship , Substrate Specificity

ABSTRACT

Subject(s)

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