کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366070 981580 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 3: Synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 3: Synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification
چکیده انگلیسی

Benzopyrans are selective estrogen receptor (ER) β agonists (SERBAs), which bind the ER subtypes α and β in opposite orientations. Here we describe the syntheses of cyclopentanone and cyclohexanone intermediates for SAR studies of the C-ring on the benzopyran scaffold. Modification of the C-ring disrupts binding to ERα, thus improving ERβ selectivity up to 100-fold. X-ray cocrystal structures confirm previously observed binding modes.

Structure activity relationship studies of the C-ring on the benzopyran scaffold are reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 17, 1 September 2007, Pages 4824–4828
نویسندگان
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