2. Academic Validation
  3. Sulfonamides as selective oestrogen receptor β agonists

Sulfonamides as selective oestrogen receptor β agonists

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5680-3. doi: 10.1016/j.bmcl.2011.08.041.
Lee R Roberts 1,  Duncan Armor,  Carolyn Barker,  Andrew Bent,  Kirstin Bess,  Alan Brown,  David A Favor,  David Ellis,  Stephen L Irving,  Malcolm MacKenny,  Chris Phillips,  Nick Pullen,  Adam Stennett,  Linda Strand,  Michelle Styles
Affiliations

Affiliation

  • 1 Worldwide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. lee.roberts@pfizer.com
PMID: 21885279 DOI: 10.1016/j.bmcl.2011.08.041
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.

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