Abstract
An oxabicyclic template for estrogen receptor alpha and beta agonists has been identified which can be tuned to provide moderate levels of selectivity for either receptor sub-type. Structure-activity relationships within this phenol-substituted oxabicyclo[3.3.1]nonene series are described. Select compounds from the present series showed activity in vivo after oral dosing in rodent models of uterine proliferation.
MeSH terms
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Administration, Oral
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Alkenes / chemistry
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Alkenes / pharmacology*
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Animals
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Bridged Bicyclo Compounds / chemistry
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Bridged Bicyclo Compounds / pharmacology*
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Dose-Response Relationship, Drug
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Estrogen Receptor alpha / agonists*
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Estrogen Receptor alpha / physiology
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Estrogen Receptor beta / agonists*
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Estrogen Receptor beta / physiology
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Female
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Models, Animal
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Molecular Conformation
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Organ Size / drug effects
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Ovariectomy
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Phenols / chemistry
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Uterus / cytology
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Uterus / drug effects
Substances
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Alkenes
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Bridged Bicyclo Compounds
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Phenols