کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1396702 1501197 2009 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Phenethyl pyridines with non-polar internal substitutents as selective ligands for estrogen receptor beta
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Phenethyl pyridines with non-polar internal substitutents as selective ligands for estrogen receptor beta
چکیده انگلیسی

To create estrogen receptor beta (ERβ)-selective ligands with improved biological characteristics, we have extended our investigations of structurally simple bibenzyl-core ligands by preparing a series of compounds in which one phenol is replaced by a 3-hydroxypyridine ring. These phenethyl pyridines were obtained by picoline anion alkylation, and compounds with different patterns of alkyl substitution on the central two carbon units were prepared. Binding affinities for ERα and ERβ were determined, and ligands with promising affinities and selectivities for ERβ were further tested for their gene transcriptional activity. Several compounds had high affinity selectivity and good potency selectivity in transcription assays. This study advances our understanding of compounds having ER-subtype selectivity and will help to direct efforts in developing novel ER ligands.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 9, September 2009, Pages 3560–3570
نویسندگان
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