Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands

  • Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. doi: 10.1016/j.bmcl.2005.08.010.
Richard Chesworth  1 ,  Matthew D Wessel ,  Lisa Heyden ,  F Michael Mangano ,  Michael Zawistoski ,  Laura Gegnas ,  David Galluzzo ,  Bruce Lefker ,  Kimberly O Cameron ,  Jeanne Tickner ,  Bihong Lu ,  Tessa A Castleberry ,  Donna N Petersen ,  Amy Brault ,  Pia Perry ,  Oicheng Ng ,  Thomas A Owen ,  Lydia Pan ,  Hua-Zhu Ke ,  Thomas A Brown ,  David D Thompson ,  Paul DaSilva-Jardine
Affiliations
  • 1. Cardiovascular and Metabolic Diseases, Medicinal Chemistry, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. [email protected]
PMID: 16219463 DOI: 10.1016/j.bmcl.2005.08.010
Abstract

A series of ligands with varying heterocyclic cores and substituents that display a range of selectivity's (up to >100x) for ER-beta over ER-alpha are reported.