Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents

…, C Cellai, A Laurenzana, S Scapecchi, F Paoletti…

Index: Guandalini; Cellai; Laurenzana; Scapecchi; Paoletti; Romanelli Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 5071 - 5074

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Citation Number: 16

Abstract

This study concerns the synthesis of new histone deacetylase inhibitors (HDACi) characterized by a 1, 4-benzodiazepine ring used as the cap, joined through an amide function or a triple bond as connection units, to a linear alkyl chain bearing the hydroxamate function as Zn2+-chelating group. Biological tests performed in human acute promyelocytic leukemia NB4 cells showed that new hybrids can induce histone H3/H4 acetylation, ...