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Bioorg Med Chem Lett. 2013 Oct 15;23(20):5571-4. doi: 10.1016/j.bmcl.2013.08.049. Epub 2013 Aug 16.

Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.

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  • 1Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, United States.

Abstract

A series of heterocyclic glucocorticoid receptor (GR) modulators with 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core are described. Structure-activity relationships suggest a combination of H-bond acceptor and a 4-fluorophenyl moiety as being important structural components contributing to the glucocorticoid receptor binding and functional activity for this series of GR modulators.

Copyright © 2013 Elsevier Ltd. All rights reserved.

KEYWORDS:

Dissociated steroids; Glucocorticoid receptor; Non-steroidal glucocorticoid receptor agonists; Transactivation; Transrepression

PMID:
24011644
[PubMed - indexed for MEDLINE]

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