Discovery of quinolines as selective glucocorticoid receptor agonists.

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Jaroch S, Berger M, Huwe C, Krolikiewicz K, Rehwinkel H, Schacke H, Schmees N, Skuballa W

Discovery of quinolines as selective glucocorticoid receptor agonists.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5835-8. doi: 10.1016/j.bmcl.2010.07.125. Epub 2010 Aug 3.

PubMed ID
20727743 [ View in PubMed
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Abstract

The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respect to inflammation endpoints, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DexamethasoneGlucocorticoid receptorEC 50 (nM)7.94N/AN/ADetails
DexamethasoneGlucocorticoid receptorIC 50 (nM)2.51N/AN/ADetails
DexamethasoneGlucocorticoid receptorIC 50 (nM)1.58N/AN/ADetails
DexamethasoneGlucocorticoid receptorIC 50 (nM)12.59N/AN/ADetails