title: Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety.
abstract: A series of novel hybrid compounds between benzofuran andN-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 derivative16not 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.
authors.affiliation: Key Laboratory of Medicinal Chemistry for Natural Resource Education Ministry, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China. 22014000171@mail.ynu.edu.cn.
authors.forename: Yulu
authors.initials: Y
authors.lastname: Ma
authors.affiliation: Central Laboratory, The No. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021, China. zhengxi138@163.com.
authors.forename: Xi
authors.initials: X
authors.lastname: Zheng
authors.affiliation: School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China. gaohui_em@126.com.
authors.forename: Hui
authors.initials: H
authors.lastname: Gao
authors.affiliation: Central Laboratory, The No. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021, China. wanchunping1012@163.com.
authors.forename: Chunping
authors.initials: C
authors.lastname: Wan
authors.affiliation: School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China. Rao_gx@163.com.
authors.forename: Gaoxiong
authors.initials: G
authors.lastname: Rao
authors.affiliation: School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China. maozw@ynutcm.edu.cn.
authors.forename: Zewei
authors.initials: Z
authors.lastname: Mao
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D051379:Mice; D009569:Nitric Oxide / Q000096:biosynthesis; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013274:Stomach Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D001572:Benzofurans; D010879:Piperazines; D009569:Nitric Oxide
keywords: N-aryl piperazine moiety; anti-inflammatory activity; anticancer activity; benzofuran