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Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety.

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 ?M), but also showed satisfactory and selective cytotoxic activity against human lung cancer line (A549) and gastric cancer cell (SGC7901) (IC50 = 0.12 ?M and 2.75 ?M, respectively), which was identified as the most potent anti-inflammatory and anti-tumor agent in this study.

SUBMITTER: Ma Y

PROVIDER: S-EPMC6274084 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety.

Ma Yulu Y Zheng Xi X Gao Hui H Wan Chunping C Rao Gaoxiong G Mao Zewei Z

Molecules (Basel, Switzerland) 20161209 12

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 ...[more]

PMID: 27941680

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