机构:[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
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.
基金:
Natural Science Foundation of China (81460624,
81560620), the Application Basic Research Program of Yunnan Province (2014FZ078, 2014FZ087) and the
Yunnan Province doctoral newcomer Award (YN2015015).
语种:
外文
PubmedID:
中科院(CAS)分区:
出版当年[2016]版:
大类|3 区化学
小类|3 区有机化学
最新[2023]版:
大类|2 区化学
小类|3 区生化与分子生物学3 区化学:综合
第一作者:
第一作者机构:[3]Key Laboratory of Medicinal Chemistry for Natural Resource Education Ministry, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China
通讯作者:
推荐引用方式(GB/T 7714):
Yulu Ma,Xi Zheng,Hui Gao,et al.Design, Synthesis, and Biological Evaluation of Novel Benzofuran Derivatives Bearing N-Aryl Piperazine Moiety[J].Molecules (Basel, Switzerland).2016,21(12):doi:10.3390/molecules21121684.