کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396702 | 1501197 | 2009 | 11 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Phenethyl pyridines with non-polar internal substitutents as selective ligands for estrogen receptor beta Phenethyl pyridines with non-polar internal substitutents as selective ligands for estrogen receptor beta](/preview/png/1396702.png)
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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Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 9, September 2009, Pages 3560–3570