1187361-06-3Relevant academic research and scientific papers
ESTROGEN RECEPTOR LIGANDS
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Page/Page column 17-18, (2010/04/06)
The invention described herein discloses bisphenol alkane compounds of formulae III and Vl and similar compounds as well as 4-[4-hydroxybenzylthio]- phenol compounds which are estrogen receptor ligands, composition containing these compounds and methods for treating various conditions using the compounds and compositions of this invention.
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta
Waibel, Michael,De Angelis, Meri,Stossi, Fabio,Kieser, Karen J.,Carlson, Kathryn E.,Katzenellenbogen, Benita S.,Katzenellenbogen, John A.
experimental part, p. 3412 - 3424 (2009/10/23)
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 gene transcription assays, some molecules showed similarly high relative transcriptional potency selectivity in favor of ERβ. Interestingly, the most ERβ-selective molecules were those bearing non-polar substituents on one of the internal carbon atoms. These compounds should be useful probes for determining the physiological roles of ERβ, and they might lead to the development of more selective and thus safer pharmaceuticals.
