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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 被引量：2

Synthesis and Bioactivity of Pyrazolo[1,5-a]pyrimidine Derivatives as Novel c-Met Inhibitors
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摘要 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. Eleven pyrazolo[1,5-a]pyrimidines were synthesized via a five-step procedure starting from 3-aminopyrazole. The structures were confirmed by IH 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）.
作者 倪春燕 张虞婷 赵育 朱俐
机构地区 南通大学航海医学研究所
出处 《有机化学》 SCIE CAS CSCD 北大核心 2012年第12期2294-2299,共6页 Chinese Journal of Organic Chemistry
基金 江苏省自然科学基金(No.BK2011390) 江苏省高校优势学科资助项目~~
关键词 吡啶并嘧啶 合成 c-Met抑制剂 抗肿瘤 pyrazolo[1,5-a]pyrimidine synthesis c-Met inhibitor anticancer
分类号 TQ464.8 [化学工程—制药化工] R914 [医药卫生—药物化学]
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参考文献17

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同被引文献22

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有机化学
2012年 第12期

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