Abstract
A series of succinimide hydroxamic acids was prepared and evaluated in vitro for HDAC inhibition and tumor cell antiproliferation. While the original macrocyclic analogue 6 was quite potent in both assays, several appropriately substituted non-macrocyclic succinimides, such as 23, were equipotent.
MeSH terms
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Amino Acids / chemistry
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Binding Sites / drug effects
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Crystallography, X-Ray
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Histone Deacetylase Inhibitors*
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Histone Deacetylases / chemistry
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Histone Deacetylases / metabolism
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Humans
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Hydroxamic Acids / chemical synthesis*
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Hydroxamic Acids / metabolism
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Hydroxamic Acids / pharmacology*
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Indicators and Reagents
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K562 Cells
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Molecular Conformation
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Structure-Activity Relationship
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Succinimides / chemical synthesis*
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Succinimides / metabolism
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Succinimides / pharmacology*
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Tumor Cells, Cultured
Substances
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Amino Acids
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Antineoplastic Agents
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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Hydroxamic Acids
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Indicators and Reagents
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Succinimides
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Histone Deacetylases