Sulfonamides as selective oestrogen receptor β agonists

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-10, Vol.21 (19), p.5680-5683
Main Authors: Roberts, Lee R., Armor, Duncan, Barker, Carolyn, Bent, Andrew, Bess, Kirstin, Brown, Alan, Favor, David A., Ellis, David, Irving, Stephen L., MacKenny, Malcolm, Phillips, Chris, Pullen, Nick, Stennett, Adam, Strand, Linda, Styles, Michelle
Format: Article
Language:English
Subjects:
agonists
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
chemistry
Drug Discovery
ERβ agonist
Estrogen Receptor alpha - metabolism
Estrogen Receptor beta - agonists
Estrogen Receptor beta - genetics
Estrogen Receptor beta - metabolism
estrogen receptors
Female
Genital system. Reproduction
Humans
Ligands
Medical sciences
Models, Chemical
Nuclear hormone receptor
Oestrogen receptor
Pharmacology. Drug treatments
Protein Binding
Structure-Activity Relationship
Sulfonamides
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - metabolism
Sulfonamides - pharmacology
X-radiation
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Description
Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.08.041