کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1363885 981524 2008 15 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and structure–activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and structure–activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group
چکیده انگلیسی

Histone deacetylase (HDAC) inhibition is a recent, clinically validated therapeutic strategy for cancer treatment. Small molecule HDAC inhibitors identified so far fall in to three distinct structural motifs: the zinc-binding group (ZBG), a hydrophobic linker, and a recognition cap group. Here we report the suitability of a 1,2,3-triazole ring as a surface recognition cap group-linking moiety in suberoylanilide hydroxamic acid-like (SAHA-like) HDAC inhibitors. Using “click” chemistry (Huisgen cycloaddition reaction), several triazole-linked SAHA-like hydroxamates were synthesized. Structure–activity relationship revealed that the position of the triazole moiety as well as the identity of the cap group markedly affected the in vitro HDAC inhibition and cell growth inhibitory activities of this class of compounds.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 9, 1 May 2008, Pages 4839–4853
نویسندگان
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