2. Academic Validation
  3. Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists

Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists

  • Bioorg Med Chem Lett. 2011 Mar 15;21(6):1697-700. doi: 10.1016/j.bmcl.2011.01.093.
Andrew R Hudson 1,  Robert I Higuchi,  Steven L Roach,  Mark E Adams,  Angela Vassar,  Peter M Syka,  Dale E Mais,  Jeffrey N Miner,  Keith B Marschke,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. andyrhudson@gmail.com
PMID: 21316964 DOI: 10.1016/j.bmcl.2011.01.093
Abstract

A series of tetrahydroquinoline derivatives were synthesized and profiled for their ability to act as Glucocorticoid Receptor selective modulators. Structure-activity relationships of the tetrahydroquinoline B-ring lead to the discovery of orally available GR-selective agonists with high in vivo activity.

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