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Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.

Research paper by Bingwei V BV Yang, Wayne W Vaccaro, Arthur M AM Doweyko, Lidia M LM Doweyko, Tram T Huynh, David D Tortolani, Steven G SG Nadler, Lorraine L McKay, John J Somerville, Deborah A DA Holloway, Sium S Habte, David S DS Weinstein, Joel C JC Barrish

Indexed on: 27 Mar '09Published on: 27 Mar '09Published in: Bioorganic & Medicinal Chemistry Letters



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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