Abstract
A novel class of phenylpyrazole fused Wieland-Miescher ketone derivatives are high affinity, receptor specific, selective modulators of glucocorticoid receptor (GR) mediated transcription in vitro, dissociating transactivation, AP-1 repression, and NF-kappaB repression from each other.
Publication types
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Research Support, U.S. Gov't, P.H.S.
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, Competitive
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Cell Line
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Fluorescence Polarization
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Humans
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In Vitro Techniques
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Ketones / chemical synthesis
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Ketones / chemistry
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Ketones / pharmacology
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Ligands
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology
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Receptors, Glucocorticoid / metabolism*
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Ketones
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Ligands
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Pyrazoles
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Receptors, Glucocorticoid