Abstract
The synthesis of a novel series of potent inhibitors of histone deacetylases is described, based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides and their derivatives. In vitro IC(50) values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC(50) of approximately 1.5 microM, comparable to or better than that of suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase currently in clinical trials.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemical synthesis*
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Amides / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Histone Deacetylase Inhibitors*
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Humans
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Sorbic Acid / analogs & derivatives*
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Sorbic Acid / chemical synthesis*
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Sorbic Acid / pharmacology
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Structure-Activity Relationship
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Sulfides / chemical synthesis*
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Sulfides / pharmacology
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Sulfinic Acids / chemical synthesis*
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Sulfinic Acids / pharmacology
Substances
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Amides
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Antineoplastic Agents
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Histone Deacetylase Inhibitors
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Sulfides
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Sulfinic Acids
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Sorbic Acid