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噻吩类氨肽酶N抑制剂的合成及初步活性

Synthesis and activities of thiophene derivate APN inhibitories

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【作者】 高凌雁卢萍李振纪穆为夏光明

【Author】 GAO Ling-yan,LU Ping,LI Zhen,JI Mu-wei,XIA Guang-ming*(School of Chemistry and Chemical Engineering,University of Jinan,Jinan 250022,China)

【机构】 济南大学化学化工学院

【摘要】 目的研究氨肽酶N抑制剂在肿瘤、癌症治疗中的作用。方法以噻吩、DMF为原料,合成2,5-噻吩二甲醛,进而合成了一系列噻吩衍生物类氨肽酶N抑制剂,并通过初步的氨肽酶活性测试。结果筛选出四种具有开发潜力的化合物。结论活性实验显示出化合物结构与活性之间存在内在关系,预计其在体内也应具有很好的抗肿瘤活性。

【Abstract】 Objective: To study the role of APN in tumor and cancer therapy.Methods: A series of thiophene derivate APN inhibitors was prepared with 2,5-thiophenedialdehyde,which was prepared with thiophene and DMF and their biological activity was tested.Results: The four compounds that had potential activities were selected.Conclusion: Biological activity tests show a relationship between the structure and activity of these compounds,and a good anti-tumor activity in bodies can also be expected.

【基金】 山东省优秀中青年科学家奖励基金(2007BS03024)
  • 【文献出处】 泰山医学院学报 ,Journal of Taishan Medical College , 编辑部邮箱 ,2009年01期
  • 【分类号】R914;R96
  • 【被引频次】4
  • 【下载频次】103
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