Abstract
A series of androstene-3,5-diene derivatives were prepared. Despite lacking the C-3 hydroxyl previously believed necessary for ER activity, some of the analogs retained surprising affinity for ER-beta. For example, diene 4 retained excellent selectivity and potency as an ER-beta agonist and was more selective for ER-beta over the androgen receptor (AR).
MeSH terms
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Androstadienes / chemical synthesis*
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Androstadienes / chemistry
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Androstadienes / pharmacology*
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Animals
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Binding Sites / drug effects
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Crystallography, X-Ray
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Estrogen Receptor beta / agonists*
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Rats
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Receptors, Androgen / drug effects
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Selective Estrogen Receptor Modulators / chemical synthesis*
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Selective Estrogen Receptor Modulators / chemistry
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Selective Estrogen Receptor Modulators / pharmacology*
Substances
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Androstadienes
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Estrogen Receptor beta
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Receptors, Androgen
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Selective Estrogen Receptor Modulators