Design and antiproliferative activity of N-heterocycle-chalcone derivatives

Design and antiproliferative activity of N-heterocycle-chalcone derivatives
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N-杂环查耳酮衍生物的设计及其抗增殖活性

DOI:
10.3184/174751916x14740355883191
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发表时间:
2016-10-01
影响因子:
1.4
通讯作者:
Zhang, Yan-Bing
Zhang, Yan-Bing
中科院分区:
化学4区
文献类型:
--
作者:
Fu, Dong-Jun;Zhang, Sai-Yang;Zhang, Yan-Bing

文献摘要

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合成了9个查尔酮类化合物,其中N-杂环化合物的氮原子连接在一个苯环上,并评价了它们对肝、胃和神经内分泌癌细胞的抗增殖活性。大多数合成的化合物对所有三种癌细胞都表现出中等到良好的活性,但特别是含有4-(咪唑-1-基)苯基和3,4,5-三甲氧基苯基的查尔酮对肝癌细胞具有最高的抗增殖活性,其IC50值为5.39μM。
Nine chalcone derivatives containing an N-heterocyclic compound attached by its nitrogen atom to one of the benzene rings were prepared and evaluated for their antiproliferative activity against liver, gastric and neuroendocrine cancer cell lines. Most of the synthesised compounds exhibited moderate to good activity against all three cancer cell lines, but in particular, a chalcone containing a 4-(imidazol-1-yl)phenyl group and a 3,4,5-trimethoxyphenyl group showed the highest antiproliferative activity with an IC50 value of 5.39 μM against liver cancer cells.