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.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / pharmacology
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Cell Line
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Drug Evaluation, Preclinical
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Genes, Reporter / genetics
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Humans
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Quinolines / chemical synthesis
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Quinolines / chemistry*
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Quinolines / pharmacology
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Receptors, Glucocorticoid / agonists*
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Receptors, Glucocorticoid / metabolism
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Transcriptional Activation
Substances
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Anti-Inflammatory Agents
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Quinolines
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Receptors, Glucocorticoid