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Updated: Jun 24, 2026

Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
Published on: September 21, 2011
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators
Bingwei V Yang1, Wayne Vaccaro, Arthur M Doweyko
1Department of Discovery Chemistry, Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543, USA. bingwei.yang@bms.com
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.
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