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

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

  • Bioorg Med Chem Lett. 2013 Oct 15;23(20):5571-4. doi: 10.1016/j.bmcl.2013.08.049.
Hai-Yun Xiao 1,  Dauh-Rurng Wu,  James E Sheppeck 2nd,  Sium F Habte,  Mark D Cunningham,  John E Somerville,  Joel C Barrish,  Steven G Nadler,  T G Murali Dhar
Affiliations

Affiliation

  • 1 Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, United States.
PMID: 24011644 DOI: 10.1016/j.bmcl.2013.08.049
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.

Keywords

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

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