2. Academic Validation
  3. Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity

Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):168-71. doi: 10.1016/j.bmcl.2010.11.047.
Steven L Roach 1,  Robert I Higuchi,  Andrew R Hudson,  Mark E Adams,  Peter M Syka,  Dale E Mais,  Jeffrey N Miner,  Keith B Marschke,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, 11085 North Torrey Pines Road, Suite 300, La Jolla, CA 92037, USA. sroach@ligand.com
PMID: 21115247 DOI: 10.1016/j.bmcl.2010.11.047
Abstract

We have previously disclosed a series of Glucocorticoid Receptor (GR) ligands derived from 6-indole-1,2,3,4-tetrahydroquinolines through structure-activity relationship (SAR) of the pendent C6-indole ring. In parallel with this effort, we now report SAR of the tetrahydroquinoline A-ring that identified the importance of a C3 hydroxyl in improving GR selectivity within a series of non-steroidal GR agonists.

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