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

Steven L Roach, Robert I Higuchi, Andrew R Hudson, Mark E Adams, Peter M Syka, Dale E Mais, Jeffrey N Miner, Keith B Marschke, Lin Zhi

Discovery Research, Ligand Pharmaceuticals, 11085 North Torrey Pines Road, Suite 300, La Jolla, CA 92037, USA. sroach@ligand.com

Bioorganic & medicinal chemistry letters 2011 Jan 1

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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. Copyright © 2010 Elsevier Ltd. All rights reserved.

Citation

Steven L Roach, Robert I Higuchi, Andrew R Hudson, Mark E Adams, Peter M Syka, Dale E Mais, Jeffrey N Miner, Keith B Marschke, Lin Zhi. Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity. Bioorganic & medicinal chemistry letters. 2011 Jan 1;21(1):168-71