title: Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
abstract: A series of dihydro-9,10-ethano-anthracene-11-carboxamides as novel glucocorticoid receptor modulators is reported. SAR exploration identified compounds from this series displaying a promising dissociation profile in discriminating between transrepression and transactivation activities. 17a is a partial agonist of GR-mediated transactivation which elicits potent and efficacious transrepression in reporter gene assays. A hypothetical binding mode is provided which accounts for the induction of functional activity by a bridgehead methyl group.
authors.affiliation: Department of Discovery Chemistry, Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543, USA. bingwei.yang@bms.com
authors.forename: Bingwei V
authors.initials: BV
authors.lastname: Yang
authors.forename: Wayne
authors.initials: W
authors.lastname: Vaccaro
authors.forename: Arthur M
authors.initials: AM
authors.lastname: Doweyko
authors.forename: Lidia M
authors.initials: LM
authors.lastname: Doweyko
authors.forename: Tram
authors.initials: T
authors.lastname: Huynh
authors.forename: David
authors.initials: D
authors.lastname: Tortolani
authors.forename: Steven G
authors.initials: SG
authors.lastname: Nadler
authors.forename: Lorraine
authors.initials: L
authors.lastname: McKay
authors.forename: John
authors.initials: J
authors.lastname: Somerville
authors.forename: Deborah A
authors.initials: DA
authors.lastname: Holloway
authors.forename: Sium
authors.initials: S
authors.lastname: Habte
authors.forename: David S
authors.initials: DS
authors.lastname: Weinstein
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish