Design, synthesis and anticancer activity of novel hybrid compounds between benzofuran and N-aryl piperazine

Design, synthesis and anticancer activity of novel hybrid compounds between benzofuran and N-aryl piperazine
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DOI:
10.1016/j.bmcl.2016.06.055
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发表时间:
2016-08-01
影响因子:
2.7
通讯作者:
Rao, Gao-Xiong
Rao, Gao-Xiong
中科院分区:
医学4区
文献类型:
--
作者:
Mao, Ze-Wei;Zheng, Xi;Rao, Gao-Xiong

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设计并合成了一系列苯并呋喃与N-芳基哌嗪的新型杂合化合物。这些衍生物进行了评估,在体外抗肿瘤活性对一组人肿瘤细胞系通过MTT测定。结果表明,酰胺类化合物比磺酰胺类化合物具有更好的生物活性,氯或三氟甲基取代基对调节细胞毒活性至关重要。特别地,发现化合物13是对4种株人肿瘤细胞系最有效的化合物,并且显示出选择性地对Hela(0.03 μ M)的细胞毒活性。(C)2016爱思唯尔有限公司版权所有
A series of novel hybrid compounds between benzofuran and N-aryl piperazine have been designed and prepared. These derivatives were evaluated for their in vitro anti-tumor activity against a panel of human tumor cell lines by MTT assay. The results demonstrated that amide derivatives were more bioactive than sulfonamide compounds in general, and that chloro or trifluoromethyl substituent was vital for modulating cytotoxic activity. In particular, compound 13 was found to be the most potent compound against 4 strains human tumor cell lines, and exhibited cytotoxic activity selectively against Hela (0.03 mu M). (C) 2016 Elsevier Ltd. All rights reserved.