کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1355502 981023 2015 13 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Development of N-hydroxybenzamide derivatives with indole-containing cap group as histone deacetylases inhibitors
چکیده انگلیسی

Histone deacetylases inhibitors (HDACIs) have captured more and more attention in many diseases therapies, of which cancer is the most intractable. A novel series of N-hydroxybenzamide derivatives containing indole cap group was designed and synthesized. Most compounds exhibited excellent HDACs inhibitory activity, especially 8q–8v with low nanomolar IC50 values (1.5–13.0 nM), which were much more potent than the positive control SAHA. The most potent compound 8r showed slightly higher growth inhibitory activity than SAHA in multiple tumor cell lines, even though, antiproliferative activity of 8r seemed inferior to its HDAC inhibition activity. Poor transcellular permeability obtained from the result of HDAC class I cellular assay could explain the inferior antiproliferative activity. In addition, 8r displayed similar HDAC IIa cellular activity to class I, which indicated 8r might be a potent pan-HDAC inhibitor.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 19, 1 October 2015, Pages 6258–6270
نویسندگان
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