Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
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.
Regan
John
J
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA. jregan@rdg.boehringer-ingelheim.com
Lee
Thomas W
TW
Zindell
Renée M
RM
Bekkali
Younes
Y
Bentzien
Jörg
J
Gilmore
Thomas
T
Hammach
Abdelhakim
A
Kirrane
Thomas M
TM
Kukulka
Alison J
AJ
Kuzmich
Daniel
D
Nelson
Richard M
RM
Proudfoot
John R
JR
Ralph
Mark
M
Pelletier
Josephine
J
Souza
Donald
D
Zuvela-Jelaska
Lijiljana
L
Nabozny
Gerald
G
Thomson
David S
DS
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
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005938:Glucocorticoids; D008070:Lipopolysaccharides; D015363:Quinolones; D018160:Receptors, Cytoplasmic and Nuclear; D015534:Trans-Activators; D003907:Dexamethasone; D001141:Aromatase