Abstract
A virtual screening approach comprising a 3-D similarity search based on known GR modulators was used to identify a novel series of non-steroidal glucocorticoid receptor (GR) antagonists. Optimization of the initial hit to provide potent compounds which exhibit good selectivity against other steroidal nuclear hormone receptors is described.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Antidepressive Agents / chemical synthesis*
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Antidepressive Agents / pharmacology
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Dose-Response Relationship, Drug
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Drug Design
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Drug Evaluation, Preclinical
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Glucocorticoids / chemistry*
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Humans
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Kinetics
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Models, Chemical
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Molecular Conformation
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Rats
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Receptors, Glucocorticoid / metabolism*
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Receptors, Steroid / metabolism
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Antidepressive Agents
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Glucocorticoids
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Receptors, Glucocorticoid
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Receptors, Steroid