- Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta
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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.
- Waibel, Michael,De Angelis, Meri,Stossi, Fabio,Kieser, Karen J.,Carlson, Kathryn E.,Katzenellenbogen, Benita S.,Katzenellenbogen, John A.
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experimental part
p. 3412 - 3424
(2009/10/23)
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- Synthesis of New Stilbene-Based Polycarbonates
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A series of polycarbonates with stilbene mesogenes has been prepared and characterized, expanding upon past work with stilbene-based polyesters and polyethers.It has been found that the stilbene mesogen, mono- or di-substituted with methyl or ethyl groups, significantly affects polymer morphology.Polycarbonates containing stilbene mesogens have been studied by differential calorimetry, polarized microscopy and X-ray diffraction.Methyl substituted stilbenes are semicrystalline and appear to be liquid crystalline, whereas ethyl substituted stilbenes are amorphous.Disubstitution lowers the transition temperatures from those values observed for monosubstituted stilbenes. - Keywords: stilbene, liquid crystal, polymer, thermotropic, amorphous, diethyl stilbestrol, x-ray diffraction, DSC, substituents
- Bluhm, A. L.,Cebe, P.,Schreuder-Gibson, H. L.,Stapler, J. T.,Yeomans, W.
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p. 123 - 140
(2007/10/02)
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