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Discovery of quinolines as selective glucocorticoid receptor agonists.
Jaroch, Stefan; Berger, Markus; Huwe, Christoph; Krolikiewicz, Konrad; Rehwinkel, Hartmut; Schäcke, Heike; Schmees, Norbert; Skuballa, Werner.
Affiliation
  • Jaroch S; Medicinal Chemistry Berlin, Lead Generation & Optimization, Bayer Schering Pharma AG, Berlin D-13342, Germany. stefan.jaroch@bayerhealthcare.com
Bioorg Med Chem Lett ; 20(19): 5835-8, 2010 Oct 01.
Article in En | MEDLINE | ID: mdl-20727743
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / Receptors, Glucocorticoid / Anti-Inflammatory Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: Germany Country of publication: United kingdom
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / Receptors, Glucocorticoid / Anti-Inflammatory Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: Germany Country of publication: United kingdom