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Bioorg Med Chem Lett. 2008 Jun 15;18(12):3504-8. doi: 10.1016/j.bmcl.2008.05.029. Epub 2008 May 11.

Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.

Author information

1
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. sroach@ligand.com

Abstract

A series of nonsteroidal glucocorticoid receptor (GR) ligands based on a 6-indole-1,2,3,4-tetrahydroquinoline scaffold are reported. Structure-activity relationship (SAR) of the pendent indole group identified compound 20 exhibiting good GR binding affinity (K(i)=1.5nM) and 100- to 1000-fold selectivity over MR, PR, and AR while showing activity in an E-selectin repression assay.

PMID:
18513967
DOI:
10.1016/j.bmcl.2008.05.029
[Indexed for MEDLINE]

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