Abstract
A series of nonsteroidal glucocorticoid receptor (GR) ligands based on a 6-indole-1,2,3,4-tetrahydroquinoline scaffold are reported. Structure-activity relationship (SAR) of the pendent indole group identified compound 20 exhibiting good GR binding affinity (K(i)=1.5nM) and 100- to 1000-fold selectivity over MR, PR, and AR while showing activity in an E-selectin repression assay.
MeSH terms
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Binding Sites
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Drug Evaluation, Preclinical
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology*
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Ligands
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Molecular Structure
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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 / drug effects*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Indoles
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Ligands
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Quinolines
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Receptors, Glucocorticoid