Abstract
Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.
MeSH terms
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Amides / chemistry*
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Amides / pharmacology*
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Animals
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Cell Line, Tumor
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Histone Deacetylase Inhibitors*
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Histone Deacetylases / metabolism
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Humans
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Mice
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Xenograft Model Antitumor Assays / methods
Substances
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Amides
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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Histone Deacetylases