Abstract
New inhibitors of histone deacetylase (HDAC) containing a sulfhydryl group were designed on the basis of the corresponding hydroxamic acid (CHAP31) and FK228. Their disulfide dimers and hybrids exhibited potent HDAC inhibitory activity in vivo with potential as anticancer prodrugs. [structure: see text]
MeSH terms
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Crystallization
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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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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Prodrugs / chemistry
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Prodrugs / pharmacology
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Sulfhydryl Compounds / chemistry
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Sulfhydryl Compounds / pharmacology*
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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Oligopeptides
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Prodrugs
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Sulfhydryl Compounds