Abstract
An optimized side chain for dihydrobenzoxathiin SERAMs was discovered and attached to four dihydrobenzoxathiin platforms. The novel SERAMs show exceptional estrogen antagonist activity in uterine tissue and an MCF-7 breast cancer cell assay.
MeSH terms
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Animals
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Breast Neoplasms / drug therapy
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Breast Neoplasms / pathology
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Estrogen Antagonists / chemical synthesis
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Estrogen Antagonists / pharmacology
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Female
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Humans
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Oxathiins / chemical synthesis*
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Oxathiins / pharmacology
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Rats
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Receptors, Estrogen / chemistry*
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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 / growth & development
Substances
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Estrogen Antagonists
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Oxathiins
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators
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dihydrobenzoxathiin