Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.
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Roach SL, Higuchi RI, Hudson AR, Adams ME, Syka PM, Mais DE, Miner JN, Marschke KB, Zhi L
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. Epub 2010 Nov 11.
- PubMed ID
- 21115247 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Prednisolone Glucocorticoid receptor EC 50 (nM) 5.3 N/A N/A Details Prednisolone Glucocorticoid receptor Ki (nM) 5.3 N/A N/A Details Prednisolone Glucocorticoid receptor IC 50 (nM) 4.1 N/A N/A Details Prednisolone Glucocorticoid receptor IC 50 (nM) 23 N/A N/A Details