Synthesis, Structural Evaluation, and Estrogen Receptor Interaction of 2,3-Diarylpiperazines

To develop novel estrogen receptor (ER) ligands, ring-fused derivatives of the hormonally active (1R,2S)/(1S,2R)-1-(2-chloro-4-hydroxyphenyl)-2-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine 4b were synthesized. (2R,3S)/(2S,3R)-2-(2-Chloro-4-hydroxyphenyl)-3-(2,6-dichloro-4-hydroxyphenyl)piperazine 4...

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Veröffentlicht in:	Journal of medicinal chemistry 2002-05, Vol.45 (11), p.2325-2337
Hauptverfasser:	Gust, Ronald, Keilitz, Roland, Schmidt, Kathrin
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding, Competitive Biological and medical sciences Cattle Cytosol - metabolism Estrogen Receptor alpha Female Gene Expression Regulation Genes, Reporter Hormones. Endocrine system In Vitro Techniques Ligands Luciferases - genetics Luciferases - metabolism Magnetic Resonance Spectroscopy Medical sciences Models, Molecular Molecular Conformation Pharmacology. Drug treatments Piperazines - chemical synthesis Piperazines - chemistry Piperazines - pharmacology Radioligand Assay Receptors, Estrogen - drug effects Receptors, Estrogen - genetics Receptors, Estrogen - metabolism Selective Estrogen Receptor Modulators - chemical synthesis Selective Estrogen Receptor Modulators - chemistry Selective Estrogen Receptor Modulators - pharmacology Structure-Activity Relationship Transcriptional Activation Tumor Cells, Cultured Uterus - ultrastructure
Online-Zugang:	Volltext
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