Abstract
A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay.
MeSH terms
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Cell Division / drug effects
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Cell Line, Tumor
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Humans
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Hydroxyquinolines / chemical synthesis
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Hydroxyquinolines / chemistry*
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Hydroxyquinolines / pharmacology*
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Inhibitory Concentration 50
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Ligands
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Receptors, Estrogen / agonists
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Receptors, Estrogen / antagonists & inhibitors
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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 / chemistry*
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Selective Estrogen Receptor Modulators / pharmacology*
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Structure-Activity Relationship
Substances
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Hydroxyquinolines
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Ligands
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators