Abstract
Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release.
MeSH terms
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Animals
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Binding Sites
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Coumarins / chemical synthesis
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Coumarins / pharmacology*
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Estradiol / chemistry
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Estradiol / pharmacology
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Estrogen Antagonists / pharmacology
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Estrogen Receptor Modulators / chemical synthesis*
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Estrogen Receptor Modulators / pharmacology
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Estrogen Receptor alpha / metabolism*
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Female
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Interleukin-6 / antagonists & inhibitors
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Interleukin-6 / metabolism*
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Molecular Structure
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Piperidines / chemical synthesis
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Piperidines / pharmacology*
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Raloxifene Hydrochloride / chemistry
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Raloxifene Hydrochloride / pharmacology
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Tamoxifen / chemistry
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Tamoxifen / pharmacology
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Tumor Cells, Cultured
Substances
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Coumarins
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Estrogen Antagonists
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Estrogen Receptor Modulators
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Estrogen Receptor alpha
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Interleukin-6
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Piperidines
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SP500263
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Tamoxifen
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Raloxifene Hydrochloride
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Estradiol