کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378246 | 981997 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
ERβ ligands. Part 5: Synthesis and structure–activity relationships of a series of 4′-hydroxyphenyl-aryl-carbaldehyde oxime derivatives
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of 4′-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high affinity (4 nM) and modest selectivity (39-fold) for estrogen receptor-β (ERβ). Substitution of one of the core rings of the scaffold based around these novel ligands further expanded our knowledge in the quest toward achieving high affinity and selectivity for ERβ. An X-ray co-crystal of structure 11 revealed that the oxime moiety was mimicking the C-ring of genistein, as previously predicted by SAR and docking studies.
A series of 4′-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high-affinity (4 nM) and modest selectivity (39-fold) for estrogen receptor-β.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 4, 15 February 2007, Pages 902–906
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 4, 15 February 2007, Pages 902–906
نویسندگان
Richard E. Mewshaw, S. Marc Bowen, Heather A. Harris, Zhang B. Xu, Eric S. Manas, Stephen T. Cohn,