Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.

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Belvedere S, Witter DJ, Yan J, Secrist JP, Richon V, Miller TA

Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3969-71. Epub 2007 Apr 29.

PubMed ID
17507219 [ View in PubMed
]
Abstract

Histone deacetylase (HDAC) inhibitors that target Class I and Class II HDACs are currently in advanced clinical trials for the treatment of cancer. Vorinostat (Zolinza, SAHA) is a hydroxamic acid approved for the treatment of patients with cutaneous T-cell lymphoma who have progressive, persistent or recurrent disease on or following two systemic therapies. As part of an on-going effort to better understand the nature of the HDAC enzyme/inhibitor interaction and design highly effective HDAC inhibitors, we herein report the design, synthesis and HDAC inhibitory activity of a vorinostat-derived series of substrate-based HDAC inhibitors.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VorinostatHistone deacetylase 1IC 50 (nM)48N/AN/ADetails