Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl) ethoxy] phenoxy]-2-(4-hydroxyphenyl)] benzo [b] thiophene: a novel, highly potent, selective estrogen …

AD Palkowitz, AL Glasebrook, KJ Thrasher…

Index: Palkowitz, Alan D.; Glasebrook, Andrew L.; Thrasher, K. Jeff; Hauser, Kenneth L.; Short, Lorri L.; Phillips, D. Lynn; Muehl, Brian S.; Sato, Masahiko; Shetler, Pamela K.; Cullinan, George J.; Pell, Tina R.; Bryant, Henry U. Journal of Medicinal Chemistry, 1997 , vol. 40, # 10 p. 1407 - 1417

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Citation Number: 185

Abstract

Raloxifene,[2-(4-hydroxyphenyl)-6-hydroxybenzo [b] thien-3-yl][4-[2-(1-piperidinyl) ethoxy] phenyl] methanone hydrochloride (2), is representative of a class of compounds known as selective estrogen receptor modulators (SERMs) that possess estrogen agonist-like actions on bone tissues and serum lipids while displaying potent estrogen antagonist properties in the breast and uterus. As part of ongoing SAR studies with raloxifene, we found that ...