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

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 demonstrat...

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Detalles Bibliográficos
Autores principales: Ma, Yulu, Zheng, Xi, Gao, Hui, Wan, Chunping, Rao, Gaoxiong, Mao, Zewei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274084/
https://www.ncbi.nlm.nih.gov/pubmed/27941680
http://dx.doi.org/10.3390/molecules21121684
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author Ma, Yulu
Zheng, Xi
Gao, Hui
Wan, Chunping
Rao, Gaoxiong
Mao, Zewei
author_facet Ma, Yulu
Zheng, Xi
Gao, Hui
Wan, Chunping
Rao, Gaoxiong
Mao, Zewei
author_sort Ma, Yulu
collection PubMed
description 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 (IC(50) = 5.28 μM), but also showed satisfactory and selective cytotoxic activity against human lung cancer line (A549) and gastric cancer cell (SGC7901) (IC(50) = 0.12 μM and 2.75 μM, respectively), which was identified as the most potent anti-inflammatory and anti-tumor agent in this study.
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spelling pubmed-62740842018-12-28 Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety Ma, Yulu Zheng, Xi Gao, Hui Wan, Chunping Rao, Gaoxiong Mao, Zewei Molecules Communication 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 (IC(50) = 5.28 μM), but also showed satisfactory and selective cytotoxic activity against human lung cancer line (A549) and gastric cancer cell (SGC7901) (IC(50) = 0.12 μM and 2.75 μM, respectively), which was identified as the most potent anti-inflammatory and anti-tumor agent in this study. MDPI 2016-12-09 /pmc/articles/PMC6274084/ /pubmed/27941680 http://dx.doi.org/10.3390/molecules21121684 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Ma, Yulu
Zheng, Xi
Gao, Hui
Wan, Chunping
Rao, Gaoxiong
Mao, Zewei
Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety
title Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety
title_full Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety
title_fullStr Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety
title_full_unstemmed Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety
title_short Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety
title_sort design, synthesis, and biological evaluation of novel benzofuran derivatives bearing n-aryl piperazine moiety
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274084/
https://www.ncbi.nlm.nih.gov/pubmed/27941680
http://dx.doi.org/10.3390/molecules21121684
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