2. Academic Validation
  3. Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity

  • J Med Chem. 2001 Aug 30;44(18):2879-85. doi: 10.1021/jm010228c.
M J Coghlan 1,  P R Kym,  S W Elmore,  A X Wang,  J R Luly,  D Wilcox,  M Stashko,  C W Lin,  J Miner,  C Tyree,  M Nakane,  P Jacobson,  B C Lane
Affiliations

Affiliation

  • 1 Pharmaceutical Products Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. coghlan_michael@lilly.com
PMID: 11520196 DOI: 10.1021/jm010228c
Abstract

A novel class of functional ligands for the human Glucocorticoid Receptor is described. Substituents in the C-10 position of the tetracyclic core are essential for Glucocorticoid Receptor (GR) selectivity versus Other steroid receptors. The C-5 position is derivatized with meta-substituted aromatic groups, resulting in analogues with a high affinity for GR (K(i) = 2.4-9.3 nM) and functional activity comparable to prednisolone in reporter gene assays of glucocorticoid-mediated gene transcription. The biological activity of these novel quinolines was also prednisolone-equivalent in whole cell assays of glucocorticoid function, and compound 13 was similar to prednisolone (po ED(50) = 2.8 mpk for 13 vs ED(50) = 1.2 mpk for prednisolone) in a rodent model of asthma (sephadex-induced eosinophil influx).

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