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Bioorg Med Chem Lett. 2013 Oct 1;23(19):5442-7. doi: 10.1016/j.bmcl.2013.06.089. Epub 2013 Jul 9.

Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.

Author information

1
Ironwood Pharmaceuticals, Cambridge, MA 02142, United States. jim.sheppeck@bms.com

Abstract

Modification of a phenolic lead structure based on lessons learned from increasing the potency of steroidal glucocorticoid agonists lead to the discovery of exceptionally potent, nonsteroidal, indazole GR agonists. SAR was developed to achieve good selectivity against other nuclear hormone receptors with the ultimate goal of achieving a dissociated GR agonist as measured by human in vitro assays. The specific interactions by which this class of compounds inhibits GR was elucidated by solving an X-ray co-crystal structure.

KEYWORDS:

Dissociated GR inhibitors; GR agonist; Glucocortocoid receptor

PMID:
23953070
DOI:
10.1016/j.bmcl.2013.06.089
[Indexed for MEDLINE]
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