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
  • 1. Worldwide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. [email protected]
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.