کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369114 981746 2015 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Benzofused hydroxamic acids: Useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-Fluorobenzothiophenes and benzofurans
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Benzofused hydroxamic acids: Useful fragments for the preparation of histone deacetylase inhibitors. Part 2: 7-Fluorobenzothiophenes and benzofurans
چکیده انگلیسی

In the search for a new class of histone deacetylase inhibitors, we prepared a series of very simple benzofused hydroxamic acids to find an anchoring fragment of minimal molecular weight: they showed very good ligand efficiencies. Following these findings, classical fragment growing work was performed to increase binding energy and selective cytotoxicity. In the second phase of the work, information from the SARs of the benzothiophene series and data available in literature, we explored the in vitro pharmacological properties of the 6-substituted-7-fluoro-benzothiophene hydroxamates and the 5-susbtituted-benzofuran hydroxamates.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 7, 1 April 2015, Pages 1603–1606
نویسندگان
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