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N-杂环取代苯并呋喃衍生物的合成及抗肿瘤活性

毛泽伟, 万春平, 姜圆, 郭文恋, 饶高雄

毛泽伟, 万春平, 姜圆, 郭文恋, 饶高雄. N-杂环取代苯并呋喃衍生物的合成及抗肿瘤活性[J]. 中国药科大学学报, 2015, 46(1): 58-61. DOI: 10.11665/j.issn.1000-5048.20150106
引用本文: 毛泽伟, 万春平, 姜圆, 郭文恋, 饶高雄. N-杂环取代苯并呋喃衍生物的合成及抗肿瘤活性[J]. 中国药科大学学报, 2015, 46(1): 58-61. DOI: 10.11665/j.issn.1000-5048.20150106
MAO Zewei, WAN Chunping, JIANG Yuan, GUO Wenlian, RAO Gaoxiong. Synthesis and anti-tumor activity in vitro of N-hetercycle substituted benzofuran derivatives[J]. Journal of China Pharmaceutical University, 2015, 46(1): 58-61. DOI: 10.11665/j.issn.1000-5048.20150106
Citation: MAO Zewei, WAN Chunping, JIANG Yuan, GUO Wenlian, RAO Gaoxiong. Synthesis and anti-tumor activity in vitro of N-hetercycle substituted benzofuran derivatives[J]. Journal of China Pharmaceutical University, 2015, 46(1): 58-61. DOI: 10.11665/j.issn.1000-5048.20150106

N-杂环取代苯并呋喃衍生物的合成及抗肿瘤活性

基金项目: 云南省应用基础研究资助项目(No.2013FZ088)

Synthesis and anti-tumor activity in vitro of N-hetercycle substituted benzofuran derivatives

  • 摘要: 为了寻找具有抗肿瘤活性的新型分子,以苯并呋喃为基础,在分子中引入N-杂环片段进行优势结构重组。以水杨醛与2-溴-4′-氟苯乙酮为原料,经取代、缩合反应后,与N-杂环化合物反应,合成10个新型N-杂环取代的苯并呋喃衍生物( 2a ~ 2j ),其结构经1H NMR、13C NMR和HRMS确证。采用MTT法初步测试了目标化合物体外抗肿瘤(HeLa,A549和H1975)活性,结果表明化合物 2a2f2j 均表现出较好的抑制活性,值得进一步深入研究。
    Abstract: To discover the novel compounds with biological activity, N-hetercycle substituted derivatives were synthesized based on the structure of benzofuran. A series of novel N-hetercycle substituted benzofuran derivatives( 2a - 2j )were synthesized by the reaction of 2-(4′-florobenzoyl)benzofuran with N-heterocyclic compounds. And the structures were characterized by 1H NMR, 13C NMR and HRMS. Their anti-tumor activities were studied in vitro against a panel of human tumor cell lines(HeLa, A549 and H1975)by the MTT assay. The results indicate that compounds 2a , 2f and 2j are the most potent within this series of compounds against human tumor cell lines, showing that they are promising lead compounds for further structural modifications and biological evaluation.
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出版历程
  • 刊出日期:  2015-02-24

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