Abstract
A series of alkylamino-2-quinolinone compounds (3) was discovered as androgen receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to androgen receptor and potent receptor modulating activities in the cotransfection assays.
MeSH terms
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Androgen Antagonists / chemical synthesis
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Androgen Antagonists / pharmacology
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Androgen Receptor Antagonists
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Androgens
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Anilides / pharmacology
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Animals
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Cell Line
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Humans
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Nitriles / pharmacology
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Quinolines / chemical synthesis
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Quinolines / chemistry*
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Quinolines / pharmacology*
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Receptors, Androgen / drug effects*
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Structure-Activity Relationship
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Tosyl Compounds / pharmacology
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Transfection
Substances
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Androgen Antagonists
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Androgen Receptor Antagonists
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Androgens
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Anilides
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Indicators and Reagents
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Nitriles
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Quinolines
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Receptors, Androgen
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Tosyl Compounds
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bicalutamide