Abstract
A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay.
MeSH terms
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Benzofurans / chemical synthesis*
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Benzofurans / pharmacology*
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Breast Neoplasms / drug therapy
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Breast Neoplasms / pathology
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Cell Line
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Drug Design
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Female
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Humans
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Models, Molecular
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Raloxifene Hydrochloride / pharmacology
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Receptors, Estrogen / drug effects
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Selective Estrogen Receptor Modulators / chemical synthesis*
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Selective Estrogen Receptor Modulators / pharmacology*
Substances
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Benzofurans
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators
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Raloxifene Hydrochloride