Abstract
A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ER alpha over ER beta, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.
MeSH terms
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Animals
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Cell Line
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Cell Proliferation / drug effects
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Female
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Heterocyclic Compounds, 4 or More Rings / chemical synthesis
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Heterocyclic Compounds, 4 or More Rings / pharmacology
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Humans
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Inhibitory Concentration 50
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Ligands
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Organ Size / drug effects
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Rats
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Receptors, Estrogen / antagonists & inhibitors*
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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 / cytology
Substances
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Heterocyclic Compounds, 4 or More Rings
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Ligands
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators