2. Academic Validation
  3. Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents

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

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5071-4. doi: 10.1016/j.bmcl.2008.07.119.
L Guandalini 1,  C Cellai,  A Laurenzana,  S Scapecchi,  F Paoletti,  M N Romanelli
Affiliations

Affiliation

  • 1 Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), University of Florence, Department of Pharmaceutical Sciences, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy.
PMID: 18723349 DOI: 10.1016/j.bmcl.2008.07.119
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, growth arrest, and also Apoptosis. Notably, chiral compounds exhibit stereoselective activity.

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