Bibenzyl-and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta

…, BS Katzenellenbogen, JA Katzenellenbogen

Index: Waibel, Michael; De Angelis, Meri; Stossi, Fabio; Kieser, Karen J.; Carlson, Kathryn E.; Katzenellenbogen, Benita S.; Katzenellenbogen, John A. European Journal of Medicinal Chemistry, 2009 , vol. 44, # 9 p. 3412 - 3424

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Citation Number: 19

Abstract

A series of structurally simple bibenzyl-diol and stilbene-diol core molecules, structural analogs of the well-known hexestrol and diethylstilbestrol non-steroidal estrogens, were prepared and evaluated as estrogen receptor (ER) subtype-selective ligands. Analysis of their ERα and ERβ binding showed that certain substitution patterns engendered binding affinities that were> 100-fold selective for ERβ. When further investigated in cell-based ...