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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 7, 1 April 2015, Pages 1603–1606
نویسندگان
Elena Marastoni, Sandra Bartoli, Marco Berettoni, Amalia Cipollone, Alessandro Ettorre, Christopher I. Fincham, Sandro Mauro, Marielle Paris, Marina Porcelloni, Mario Bigioni, Monica Binaschi, Federica Nardelli, Massimo Parlani, Carlo A. Maggi,