| Literature DB >> 24011644 |
Hai-Yun Xiao1, Dauh-Rurng Wu, James E Sheppeck, Sium F Habte, Mark D Cunningham, John E Somerville, Joel C Barrish, Steven G Nadler, T G Murali Dhar.
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.Entities:
Keywords: Dissociated steroids; Glucocorticoid receptor; Non-steroidal glucocorticoid receptor agonists; Transactivation; Transrepression
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Year: 2013 PMID： 24011644 DOI： 10.1016/j.bmcl.2013.08.049
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823