Abstract
A series of p-hydroxybenzenesulphonamides ERβ receptor agonists were discovered and several compounds identified had excellent selectivity over the related ERα receptor. One of these, compound 11, had an interesting binding conformation determined by X-ray and represents an excellent starting point in the quest for further selective ERβ agonists.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Drug Discovery*
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Estrogen Receptor alpha / metabolism
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Estrogen Receptor beta / agonists*
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Estrogen Receptor beta / genetics
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Estrogen Receptor beta / metabolism
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Female
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Humans
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Ligands
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Models, Chemical
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Protein Binding
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / metabolism
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Sulfonamides / pharmacology*
Substances
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ESR1 protein, human
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Ligands
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Sulfonamides