Article ID Journal Published Year Pages File Type
1377345 Bioorganic & Medicinal Chemistry Letters 2008 5 Pages PDF
Abstract

Inhibition of histone deacetylases (HDAC) is emerging as a new strategy in human cancer therapy. The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides is presented herein. From the different series bearing a six-membered heteroaromatic ring studied, the s-triazine series showed the best HDAC1 enzyme and in vitro anti-proliferative activities with IC50 values below micromolar range. Some of these compounds can also significantly reduce tumor growth in human tumor xenograft models in mice.

Graphical abstractThe synthesis and biological evaluation as histone deacetylase (HDACs) inhibitors of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides of the general structure shown is presented herein.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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