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Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands
Authors:Chesworth Richard  Wessel Matthew D  Heyden Lisa  Mangano F Michael  Zawistoski Michael  Gegnas Laura  Galluzzo David  Lefker Bruce  Cameron Kimberly O  Tickner Jeanne  Lu Bihong  Castleberry Tessa A  Petersen Donna N  Brault Amy  Perry Pia  Ng Oicheng  Owen Thomas A  Pan Lydia  Ke Hua-Zhu  Brown Thomas A  Thompson David D  DaSilva-Jardine Paul
Institution:

aCardiovascular and Metabolic Diseases, Medicinal Chemistry, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA

bComputational Chemistry, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA

cCardiovascular and Metabolic Diseases, Biology, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA

Abstract:A series of ligands with varying heterocyclic cores and substituents that display a range of selectivity’s (up to >100x) for ER-β over ER-greek small letter alpha are reported.
Keywords:Estrogen receptor  ER beta selective ligands
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