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Bioorg Med Chem Lett. 2009 Apr 15;19(8):2139-43. doi: 10.1016/j.bmcl.2009.03.006. Epub 2009 Mar 9.

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

Author information

1
Department 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.

PMID:
19321341
DOI:
10.1016/j.bmcl.2009.03.006
[Indexed for MEDLINE]

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