Abstract
We report the preparation and structure-activity relationships of phosphorus-containing histone deacetylase inhibitors. A strong trend between decreasing phosphorus functional group size and superior mouse pharmacokinetic properties was identified. In addition, optimized candidates showed tumor growth inhibition in xenograft studies.
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacokinetics*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacokinetics*
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Histone Deacetylase 1
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Histone Deacetylase 2
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Histone Deacetylase Inhibitors*
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Histone Deacetylases / metabolism
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Mice
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Mice, Nude
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Organophosphonates / chemical synthesis
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Organophosphonates / chemistry
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Organophosphonates / pharmacokinetics*
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Repressor Proteins / antagonists & inhibitors*
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Repressor Proteins / metabolism
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Transplantation, Heterologous
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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Organophosphonates
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Repressor Proteins
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Hdac1 protein, mouse
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Hdac2 protein, mouse
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Histone Deacetylase 1
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Histone Deacetylase 2
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Histone Deacetylases