title: Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3β.
abstract: 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.
authors.affiliation: ActivX Biosciences, Inc., 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Oana M
authors.initials: OM
authors.lastname: Cociorva
authors.forename: Bei
authors.initials: B
authors.lastname: Li
authors.forename: Tyzoon
authors.initials: T
authors.lastname: Nomanbhoy
authors.forename: Qiang
authors.initials: Q
authors.lastname: Li
authors.forename: Ayako
authors.initials: A
authors.lastname: Nakamura
authors.forename: Kai
authors.initials: K
authors.lastname: Nakamura
authors.forename: Masahiro
authors.initials: M
authors.lastname: Nomura
authors.forename: Kyoko
authors.initials: K
authors.lastname: Okada
authors.forename: Shigeki
authors.initials: S
authors.lastname: Seto
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Yumoto
authors.forename: Marek
authors.initials: M
authors.lastname: Liyanage
authors.forename: Melissa C
authors.initials: MC
authors.lastname: Zhang
authors.forename: Arwin
authors.initials: A
authors.lastname: Aban
authors.forename: Brandon
authors.initials: B
authors.lastname: Leen
authors.forename: Anna Katrin
authors.initials: AK
authors.lastname: Szardenings
authors.forename: Jonathan S
authors.initials: JS
authors.lastname: Rosenblum
authors.forename: John W
authors.initials: JW
authors.lastname: Kozarich
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Kohno
authors.forename: Kevin R
authors.initials: KR
authors.lastname: Shreder
mesh_terms: D042462:4-Quinolones / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002986:Clinical Trials as Topic; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000071679:Glycogen Synthase Kinase 3 beta; D018922:HL-60 Cells; D057166:High-Throughput Screening Assays; D006801:Humans; D020128:Inhibitory Concentration 50; D007527:Isoenzymes; D058990:Molecular Targeted Therapy; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D042462:4-Quinolones; D000900:Anti-Bacterial Agents; D007527:Isoenzymes; D047428:Protein Kinase Inhibitors; C000605506:GSK3B protein, human; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3