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

Richard Chesworth; 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

doi:10.1016/j.bmcl.2005.08.010

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. Epub 2005 Oct 10.

Affiliation

¹ Cardiovascular and Metabolic Diseases, Medicinal Chemistry, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. rchesworth@gmail.com

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.

Publication types

Comparative Study

MeSH terms

Cell Line, Tumor
Crystallography, X-Ray
Estrogen Receptor alpha / metabolism
Estrogen Receptor beta / chemistry
Estrogen Receptor beta / metabolism*
Heterocyclic Compounds / chemical synthesis
Heterocyclic Compounds / pharmacokinetics*
Humans
Indicators and Reagents
Kinetics
Ligands
Selective Estrogen Receptor Modulators / chemistry
Structure-Activity Relationship

Substances

Estrogen Receptor alpha
Estrogen Receptor beta
Heterocyclic Compounds
Indicators and Reagents
Ligands
Selective Estrogen Receptor Modulators