Abstract
Three novel structural motifs based on a bicyclo [3.3.1]nonane template were examined as new ligands for estrogen receptor (ER). Type III compounds emerged as the most promising leads for developing high-affinity ER ligands, but they showed little selectivity for either ER subtype. Type II compounds, on the other hand, despite their lower affinity, exhibited significant ERbeta binding selectivity.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkanes / chemical synthesis
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Alkanes / chemistry
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Alkanes / pharmacology*
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Animals
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / chemistry
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Bridged Bicyclo Compounds / pharmacology*
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Bridged-Ring Compounds / chemical synthesis
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Bridged-Ring Compounds / chemistry
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Bridged-Ring Compounds / pharmacology*
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Cyclofenil / metabolism
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Female
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Indicators and Reagents
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Kinetics
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Ligands
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Models, Molecular
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Molecular Structure
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Radioligand Assay
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Receptors, Estrogen / drug effects
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Receptors, Estrogen / metabolism*
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Alkanes
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Bridged Bicyclo Compounds
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Bridged-Ring Compounds
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Indicators and Reagents
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Ligands
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Receptors, Estrogen
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bicyclo(3.3.1)nonane
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Cyclofenil
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nonane