- 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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- Preparation of 1,2-bis(4-hydroxyphenyl)-2-hydroxypropanes
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The present invention relates to the preparation of substituted or unsubstituted 1,2-bis(4-hydroxyphenyl)-hydroxyaliphatics such as 1,2-bis(4-hydroxyphenyl)-2-hydroxypropanes by reacting substituted or unsubstituted 1,2-bis(4-hydroxyphenyl)-halogen substituted aliphatics such as 1,2-bis(4-hydroxyphenyl)-2-chloropropanes in the presence of a base and water.
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- Preparation of 4,4'-dihydroxy-'alkylstiblbene with reduced dimer formation
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Preparation of dihydroxy-α-alkylstilbenes with reduced undesirable by-products can be achieved by carrying out dehydrohalogenation of a substantially uniform dispersion of a halogenated intermediate of the desired product in the presence of water and a polar protic solvent.
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- Rodlike mesogenic thiirane resins (polythiiranes)
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Polythiirane resins are disclosed which contain at least one, rodlike mesogenic moiety. These resins can be cured by conventional curing agents typically employed to cure epoxy resins or they can be thermally cured without a curing agent.
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- Diglycidyl ether of 4,4'-dihydroxy-α-methylstilbene
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The diglycidyl ether of 4,4'-dihydroxy-α-methylstilbene is prepared.
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- Bis(aminophenoxy)-alpha-substituted stilbenes
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bis(Aminophenoxy)-alpha-substituted stilbenes are prepared by reacting a dihydroxy-alpha-substituted stilbene with a halonitrobenzene in the presence of a basic acting substance such as potassium carbonate and hydrogenating the resulting bis(nitrophenoxy)-alpha-substituted stilbene to convert the nitro groups to amino groups. These compounds are useful as curing agents for epoxy resins.
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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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- Sulfonamide compounds containing mesogenic moieties
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Adducts containing mesogenic or rodlike moieties are prepared by reacting (1) at least one compound containing an average of more than one vicinal epoxide group per molecule with (2) at least one compound containing an average of more than one reactive hydrogen atom per molecule; with the proviso that at least one member of components (1) and (2) contains a mesogenic or rodlike moiety. These compounds are useful as curing agents for epoxy resins.
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- Polymer modified adducts of epoxy resins and active hydrogen containing compounds containing mesogenic moieties
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Polymer modified adducts are prepared by (A) reacting (1) an epoxy resin having an average of more than one vicinal epoxide group with (2) a compound containing an average of two or more hydrogen atoms reactive with an epoxide group; and (B) partially vinylizing reacting the product from step (A); and (C) polymerizing the partially vinylized product from step (B) with (3) a polymerizable ethylenically unsaturated monomer; with the proviso that at least one of the components (1), (2) or (3) contain one or more mesogenic or rodlike moieties. These adducts are useful as epoxy resin curing agents.
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