Abstract
We synthesized a series of delta-lactam-based HDAC inhibitors that were identified with various degrees of anti-inflammatory and cell growth inhibitory activities. Compounds possessing significant HDAC inhibitory activity exhibited both anti-inflammatory and cell growth inhibitory activities as well as significant tumor growth inhibition in the in vivo tumor xenograft experiments. Besides, these compounds demonstrated anti-inflammatory properties in vitro via suppression of the production of the proinflammatory cytokine TNF-alpha and nitric oxide by LPS-stimulated RAW264.7 cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Line
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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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Lactams / chemical synthesis*
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Lactams / chemistry
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Lactams / pharmacology
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Lipopolysaccharides / pharmacology
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Mice
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Models, Molecular
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Nitric Oxide / antagonists & inhibitors
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Nitric Oxide / biosynthesis
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Structure-Activity Relationship
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Transplantation, Heterologous
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Tumor Necrosis Factor-alpha / biosynthesis
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Antineoplastic Agents
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Histone Deacetylase Inhibitors
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Lactams
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Lipopolysaccharides
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Tumor Necrosis Factor-alpha
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Nitric Oxide