title: Identification of dissociated non-steroidal glucocorticoid receptor agonists.
abstract: A new series of ligands for the glucocorticoid receptor (GR) is described. SAR development was guided by docking 3 into the GR active site and optimizing an unsubstituted phenyl ring for key interactions found in the steroid A-ring binding pocket. To identify compounds with an improved side effect profile over marketed steroids the functional activity of compounds was evaluated in cell based assays for transactivation (aromatase) and transrepression (IL-6). Through this effort, 36 has been identified as a partial agonist with a dissociated profile in these cell based assays.
authors: Medicinal Chemistry Department, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA. dkuzmich@rdg.boehringer-ingelheim.com
authors: Daniel
authors: D
authors: Kuzmich
authors: Tom
authors: T
authors: Kirrane
authors: John
authors: J
authors: Proudfoot
authors: Younes
authors: Y
authors: Bekkali
authors: Renee
authors: R
authors: Zindell
authors: Laura
authors: L
authors: Beck
authors: Richard
authors: R
authors: Nelson
authors: Cheng-Kon
authors: CK
authors: Shih
authors: Alison J
authors: AJ
authors: Kukulka
authors: Zofia
authors: Z
authors: Paw
authors: Patty
authors: P
authors: Reilly
authors: Rodney
authors: R
authors: Deleon
authors: Mario
authors: M
authors: Cardozo
authors: Gerald
authors: G
authors: Nabozny
authors: David
authors: D
authors: Thomson
mesh_terms: D005938:Glucocorticoids / Q000819:agonists*; D008024:Ligands; D008958:Models, Molecular; D013329:Structure-Activity Relationship
chemical_list: D005938:Glucocorticoids; D008024:Ligands