D. Stolfa, A. Stefanachi, Julia M. Gajer
Jul 1, 2012
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Influential Citations
15
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Quality indicators
Journal
ChemMedChem
Abstract
Epigenetic regulation is an essential process for the normal functioning of genes. Therefore, targeting epigenetic dysregulation in cancer may be a valid therapeutic approach for the treatment of this severe disease. Histone deacetylases (HDACs) are enzymes involved in the regulation of epigenetic post‐translational modifications; because they are overexpressed in many types of cancer, HDACs are valuable targets for the development of new anticancer agents. A large series of 2‐aminobenzanilides linked at the 4′‐position to α‐amino acid amides, arenes, and heteroarenes through a methylene bridge were designed, synthesized, and tested as novel HDAC inhibitors. Several compounds showed IC50 values in the two‐digit nanomolar range in hrHDAC1 inhibition assays, lower than that of the reference compound MS‐275. They also showed interesting selectivity profiles, as confirmed by western blot assays.