Abstract
Several tetrahydrofluorenones with a triazole fused across C7-C8 showed high levels of ERbeta-selectivity and were found to be potent ERbeta-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERbeta.
MeSH terms
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Animals
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Azo Compounds / chemical synthesis*
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Azo Compounds / chemistry
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Azo Compounds / pharmacokinetics
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Azo Compounds / pharmacology*
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Estrogen Receptor beta / agonists*
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Estrogen Receptor beta / metabolism
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Fluorenes / chemical synthesis
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Fluorenes / chemistry*
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Fluorenes / pharmacokinetics
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Fluorenes / pharmacology*
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Humans
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Ligands
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Molecular Structure
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Rats
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Structure-Activity Relationship
Substances
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Azo Compounds
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Estrogen Receptor beta
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Fluorenes
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Ligands
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fluorene