Abstract
We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic activity against a range of human tumor-derived cell lines. KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or i.v. dose and inhibition of tumor growth following chronic dosing.
MeSH terms
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Animals
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Antineoplastic Agents / chemistry
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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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Enzyme Inhibitors / pharmacology*
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HCT116 Cells
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Histone Deacetylase Inhibitors*
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Humans
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Inhibitory Concentration 50
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Mice
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Mice, Nude
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Molecular Structure
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Prodrugs / chemistry
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Prodrugs / pharmacology*
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Pyridines / chemistry
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Pyridines / pharmacology*
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Structure-Activity Relationship
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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KD 5170
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Prodrugs
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Pyridines
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Sulfonamides