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Molecules 2016, 21(12), 1684; doi:10.3390/molecules21121684

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

1
School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China
2
Central Laboratory, The No. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021, China
3
Key Laboratory of Medicinal Chemistry for Natural Resource Education Ministry, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 6 October 2016 / Revised: 27 November 2016 / Accepted: 1 December 2016 / Published: 9 December 2016
(This article belongs to the Section Medicinal Chemistry)
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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. View Full-Text
Keywords: benzofuran; N-aryl piperazine moiety; anti-inflammatory activity; anticancer activity benzofuran; N-aryl piperazine moiety; anti-inflammatory activity; anticancer activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Ma, Y.; Zheng, X.; Gao, H.; Wan, C.; Rao, G.; Mao, Z. Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety. Molecules 2016, 21, 1684.

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