کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364344 981535 2008 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors
چکیده انگلیسی

Trifluoroacetylthiophene carboxamides have recently been reported to be class II HDAC inhibitors, with moderate selectivity. Exploration of replacements for the carboxamide with bioisosteric pentatomic heteroaromatic like 1,3,4-oxadiazoles, 1,2,4-oxadiazoles and 1,3-thiazoles, led to the discovery that 2-trifluoroacetylthiophene 1,3,4-oxadiazole derivatives are very potent low nanomolar HDAC4 inhibitors, highly selective over class I HDACs (HDAC 1 and 3), and moderately stable in HCT116 cell culture.

Replacement of the carboxamide moiety of trifluoroacetylthiophene HDAC4 inhibitors with bioisosteric pentatomic heteroaromatics led to the discovery of a novel series of potent and highly selective low nanomolar class II HDAC inhibitors.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 23, 1 December 2008, Pages 6083–6087
نویسندگان
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