title: Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
abstract: We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.
authors.affiliation: Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA. jregan@rdg.boehringer-ingelheim.com
authors.forename: John
authors.initials: J
authors.lastname: Regan
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Lee
authors.forename: Renée M
authors.initials: RM
authors.lastname: Zindell
authors.forename: Younes
authors.initials: Y
authors.lastname: Bekkali
authors.forename: Jörg
authors.initials: J
authors.lastname: Bentzien
authors.forename: Thomas
authors.initials: T
authors.lastname: Gilmore
authors.forename: Abdelhakim
authors.initials: A
authors.lastname: Hammach
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Kirrane
authors.forename: Alison J
authors.initials: AJ
authors.lastname: Kukulka
authors.forename: Daniel
authors.initials: D
authors.lastname: Kuzmich
authors.forename: Richard M
authors.initials: RM
authors.lastname: Nelson
authors.forename: John R
authors.initials: JR
authors.lastname: Proudfoot
authors.forename: Mark
authors.initials: M
authors.lastname: Ralph
authors.forename: Josephine
authors.initials: J
authors.lastname: Pelletier
authors.forename: Donald
authors.initials: D
authors.lastname: Souza
authors.forename: Lijiljana
authors.initials: L
authors.lastname: Zuvela-Jelaska
authors.forename: Gerald
authors.initials: G
authors.lastname: Nabozny
authors.forename: David S
authors.initials: DS
authors.lastname: Thomson
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001141:Aromatase / Q000378:metabolism; D003907:Dexamethasone / Q000494:pharmacology; D005260:Female; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D005938:Glucocorticoids / Q000819:agonists*; D006367:HeLa Cells; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D008807:Mice, Inbred BALB C; D018716:Molecular Mimicry; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism*; D015534:Trans-Activators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015533:Transcriptional Activation
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005938:Glucocorticoids; D008070:Lipopolysaccharides; D015363:Quinolones; D018160:Receptors, Cytoplasmic and Nuclear; D015534:Trans-Activators; D003907:Dexamethasone; D001141:Aromatase