Abstract
A novel series of 17beta-hydroxysteroid dehydrogenase type 3 (17beta-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17beta-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays.
MeSH terms
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17-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
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17-Hydroxysteroid Dehydrogenases / metabolism
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Alkaline Phosphatase / drug effects
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Alkaline Phosphatase / metabolism
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Androstenedione / metabolism
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Azocines* / chemical synthesis
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Azocines* / chemistry
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Azocines* / pharmacology
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Enzyme Inhibitors* / chemical synthesis
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Enzyme Inhibitors* / chemistry
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Enzyme Inhibitors* / pharmacology
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Humans
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Models, Molecular
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Molecular Structure
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Structure-Activity Relationship
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Testosterone / biosynthesis
Substances
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Azocines
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Enzyme Inhibitors
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Testosterone
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Androstenedione
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17-Hydroxysteroid Dehydrogenases
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17beta-hydroxysteroid dehydrogenase type 3
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Alkaline Phosphatase