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

Autor:	Kevin R. Shreder, Tyzoon K. Nomanbhoy, Ayako Nakamura, Anna Katrin Szardenings, Shigeki Seto, Jonathan S. Rosenblum, Brandon Leen, Oana Cociorva, Kai Nakamura, Bei Li, Marek Liyanage, John W. Kozarich, Qiang Li, Yasushi Kohno, Kazuhiro Yumoto, Kyoko Okada, Masahiro Nomura, Melissa C. Zhang, Arwin Aban
Rok vydání:	2011
Předmět:	Stereochemistry Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science HL-60 Cells Biochemistry Isozyme Substrate Specificity Glycogen Synthase Kinase 3 Inhibitory Concentration 50 Structure-Activity Relationship GSK-3 Drug Discovery Humans Structure–activity relationship heterocyclic compounds Molecular Targeted Therapy Glycogen synthase Protein Kinase Inhibitors Molecular Biology GSK3B chemistry.chemical_classification Clinical Trials as Topic 4-Quinolones Glycogen Synthase Kinase 3 beta biology Bicyclic molecule Kinase Organic Chemistry Anti-Bacterial Agents High-Throughput Screening Assays Isoenzymes chemistry Drug Design biology.protein Molecular Medicine Tricyclic
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:5948-5951
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9d9755d781aad544131d0a6c744f45f https://doi.org/10.1016/j.bmcl.2011.07.073 Zobrazit plný text záznamu Full Text from ScienceDirect