Abstract
A series of novel hybrid compounds between benzofuran and N-aryl piperazine have been synthesized and screened in vitro for anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and for anticancer activity against three human tumor cell lines. The results demonstrated that derivative 16 not only had inhibitory effect on the generation of NO (IC50 = 5.28 μM), but also showed satisfactory and selective cytotoxic activity against human lung cancer line (A549) and gastric cancer cell (SGC7901) (IC50 = 0.12 μM and 2.75 μM, respectively), which was identified as the most potent anti-inflammatory and anti-tumor agent in this study.
Keywords:
N-aryl piperazine moiety; anti-inflammatory activity; anticancer activity; benzofuran.
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / 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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Benzofurans* / chemical synthesis
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Benzofurans* / chemistry
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Benzofurans* / pharmacology
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Humans
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Lung Neoplasms / drug therapy*
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Lung Neoplasms / metabolism
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Lung Neoplasms / pathology
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Mice
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Nitric Oxide / biosynthesis
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Piperazines* / chemical synthesis
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Piperazines* / chemistry
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Piperazines* / pharmacology
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Stomach Neoplasms / drug therapy*
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Stomach Neoplasms / metabolism
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Stomach Neoplasms / pathology
Substances
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Anti-Inflammatory Agents
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Antineoplastic Agents
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Benzofurans
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Piperazines
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Nitric Oxide