Abstract
Dihydrobenzodithiin compounds (1-6) were prepared to explore the expansion of the dihydrobenzoxathiin lead compounds I-III as SERAMs (Selective Estrogen Receptor Alpha Modulators). The dihydrobenzodithiin compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, however, they lacked the in vivo antagonism/agonism activity exhibited by the lead class in an immature rat uterine growth model.
MeSH terms
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Animals
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Binding Sites
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Cells, Cultured
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Female
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Heterocyclic Compounds, 2-Ring / chemical synthesis*
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Heterocyclic Compounds, 2-Ring / pharmacology
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Inhibitory Concentration 50
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Ligands
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Models, Biological
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Piperidines / chemical synthesis*
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Piperidines / pharmacology
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Rats
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Receptors, Estrogen / metabolism*
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Selective Estrogen Receptor Modulators / chemical synthesis*
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Selective Estrogen Receptor Modulators / pharmacology
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Structure-Activity Relationship
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Uterus / drug effects
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Uterus / metabolism
Substances
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Heterocyclic Compounds, 2-Ring
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Ligands
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Piperidines
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators