Abstract
Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic “histone code,” thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overview describes the chemistry and preliminary characterization of recently disclosed molecules in three major classes of HDAC inhibitors: hydroxamic acids, 2-aminobenzanilides, and cyclic peptides. In addition, results from recent clinical trials on isotype-selective HDAC inhibitors are reviewed. It is clear from the plethora of new molecules and the encouraging results from clinical trials that HDAC inhibitors hold a great deal of promise, particularly as add-on therapy, for the treatment of a variety of solid and hematologic cancers.
Keywords: Acetylation, antineoplastic agent, clinical trials, histone deacetylases, histones, apoptosis, cell-cycle arrest
Current Topics in Medicinal Chemistry
Title: Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents
Volume: 8 Issue: 10
Author(s): Oscar Moradei, Arkadii Vaisburg and Robert E. Martell
Affiliation:
Keywords: Acetylation, antineoplastic agent, clinical trials, histone deacetylases, histones, apoptosis, cell-cycle arrest
Abstract: Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic “histone code,” thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overview describes the chemistry and preliminary characterization of recently disclosed molecules in three major classes of HDAC inhibitors: hydroxamic acids, 2-aminobenzanilides, and cyclic peptides. In addition, results from recent clinical trials on isotype-selective HDAC inhibitors are reviewed. It is clear from the plethora of new molecules and the encouraging results from clinical trials that HDAC inhibitors hold a great deal of promise, particularly as add-on therapy, for the treatment of a variety of solid and hematologic cancers.
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Cite this article as:
Moradei Oscar, Vaisburg Arkadii and Martell E. Robert, Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents, Current Topics in Medicinal Chemistry 2008; 8 (10) . https://dx.doi.org/10.2174/156802608784911581
DOI https://dx.doi.org/10.2174/156802608784911581 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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