Sulfonamides as selective oestrogen receptor beta agonists.

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Roberts LR, Armor D, Barker C, Bent A, Bess K, Brown A, Favor DA, Ellis D, Irving SL, MacKenny M, Phillips C, Pullen N, Stennett A, Strand L, Styles M

Sulfonamides as selective oestrogen receptor beta agonists.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5680-3. doi: 10.1016/j.bmcl.2011.08.041. Epub 2011 Aug 16.

PubMed ID

21885279 [ View in PubMed

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Abstract

A series of p-hydroxybenzenesulphonamides ERbeta receptor agonists were discovered and several compounds identified had excellent selectivity over the related ERalpha 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 ERbeta agonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor alpha	EC 50 (nM)	0.046	N/A	N/A	Details
Estradiol	Estrogen receptor beta	EC 50 (nM)	0.25	N/A	N/A	Details