有机化学 ›› 2012, Vol. 32 ›› Issue (12): 2294-2299.DOI: 10.6023/cjoc201207010 上一篇    下一篇

研究论文

吡唑并[1,5-a]嘧啶类c-Met激酶抑制剂的合成及生物活性研究

倪春燕, 张虞婷, 赵育, 朱俐   

  1. 南通大学航海医学研究所 南通 226001
  • 收稿日期:2012-07-12 修回日期:2012-08-21 发布日期:2012-08-27
  • 通讯作者: 赵育 E-mail:zhaoyoo@163.com
  • 基金资助:
    江苏省自然科学基金(No. BK2011390)和江苏省高校优势学科资助项目.

Synthesis and Bioactivity of Pyrazolo[1,5-a]pyrimidine Derivatives as Novel c-Met Inhibitors

Ni Chunyan, Zhang Yuting, Zhao Yu, Zhu Li   

  1. Institute of Nautical Medicine, Nantong University, Nantong 226001
  • Received:2012-07-12 Revised:2012-08-21 Published:2012-08-27
  • Supported by:
    Project supported by the Natural Science Foundation of Jiangsu Province (No. BK2011390) and the Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD).

设计并合成了5,6-二甲基-7-(2-氟-4-氨基苯氧基)吡唑并[1,5-a]嘧啶类c-Met激酶抑制剂. 以3-氨基吡唑和2-甲 基-乙酰乙酸乙酯为起始原料, 经5步反应合成了11个未见文献报道的吡唑并[1,5-a]嘧啶类衍生物, 通过氢谱、碳谱、高分辨质谱等方法对所合成的化合物进行了结构表征. 采用噻唑蓝法(MTT)的方法和酶联免疫吸附测定(ELISA)方法检测部分新化合物的生物活性.

关键词: 吡啶并嘧啶, 合成, c-Met抑制剂, 抗肿瘤

Eleven pyrazolo[1,5-a]pyrimidines were synthesized via a five-step procedure starting from 3-aminopyrazole. The structures were confirmed by 1H NMR, 13C NMR and HRMS techniques. Their antiproliferative activities against A549 cell line were investigated by methyl thiazolyl tetrazoliym (MTT) assay. Their c-Met kinase inhibitory abilities were evaluated by using enzyme-linked immunosorbent assay (ELISA).

Key words: pyrazolo[1,5-a]pyrimidine, synthesis, c-Met inhibitor, anticancer