کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1379370 982027 2005 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Exploring the connection unit in the HDAC inhibitor pharmacophore model: Novel uracil-based hydroxamates
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Exploring the connection unit in the HDAC inhibitor pharmacophore model: Novel uracil-based hydroxamates
چکیده انگلیسی

Starting from the pharmacophore model for HDAC inhibitor design, a novel series of hydroxamates bearing a uracil moiety as connecting unit (CU) has been prepared and tested. Almost all compounds exhibited HDAC inhibiting activity at low nanomolar concentrations, the N-hydroxy-6-(3,4-dihydro-4-oxo-6-benzyl- and -6-phenyl-2-pyrimidinylthio)hexanamides 1d and 1l being more potent than SAHA in enzymatic assays. Such compounds also caused hyperacetylation in NIH3T3 cell core histones and were endowed with interesting antiproliferative and cytodifferentiating effects in human leukemia (HL-60) cells.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 21, 1 November 2005, Pages 4656–4661
نویسندگان
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