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Bioorg Med Chem Lett. 2011 Mar 15;21(6):1654-7. doi: 10.1016/j.bmcl.2011.01.104. Epub 2011 Jan 27.

Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.

Author information

1
Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. andyrhudson@gmail.com

Abstract

Continuing studies based on dihydroquinoline glucocorticoid receptor agonists lead to the discovery of a series of C4-oxime analogs. Representative compounds exhibited potent transrepression activity with minimal transactivation of phosphoenolpyruvate caboxykinase (PEPCK), a key protein in the gluconeogenesis pathway. These compounds represent promising leads in identifying GR agonists with high anti-inflammatory activity and attenuated potential for glucose elevation.

PMID:
21324689
DOI:
10.1016/j.bmcl.2011.01.104
[Indexed for MEDLINE]

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