کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371744 981853 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity
چکیده انگلیسی

A series of N-hydroxy-3-[3-(1-substituted-1H-benzoimidazol-2-yl)-phenyl]-acrylamides (5a–5ab) and N-hydroxy-3-[3-(1,4,5-trisubstituted-1H-imidazol-2-yl)-phenyl]-acrylamides (12a–s) were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases. Multiple compounds bearing an N1-piperidine demonstrate EC50s of 20–100 nM in human A549, HL60, and PC3 cells, in vitro and in vivo hyperacetylation of histones H3 and H4, and induction of p21waf. Compound 5x displays efficacy in human tumor xenograft models.

A series of imidazole and benzimidazole compounds were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases, displaying activity in cellular and xenograft models.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 10, 15 May 2010, Pages 3138–3141
نویسندگان
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