Abstract
Compounds were synthesized where oxygen in the ethoxypiperidine region of raloxifene is replaced with carbon, sulfur, or nitrogen linkages. Thia- and aza-substituted compounds were prepared by novel methodology. The compounds were evaluated in vitro as selective estrogen receptor modulators (SERMs). Calculations suggested the compounds exhibit an ER-alpha binding affinity/conformational energy relationship.
MeSH terms
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Binding, Competitive
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Carbon / chemistry*
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Cell Division / drug effects
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Cell Line
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Crystallography, X-Ray
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Humans
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Oxygen / chemistry*
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Piperidines / chemistry*
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Piperidines / metabolism
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Piperidines / pharmacology*
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Raloxifene Hydrochloride
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Receptors, Estrogen / drug effects*
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Receptors, Estrogen / metabolism
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Structure-Activity Relationship
Substances
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Piperidines
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Receptors, Estrogen
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Raloxifene Hydrochloride
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Carbon
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Oxygen