水杨酰芳胺类化合物的设计、合成及体外抗肿瘤活性研究有机化学.pdfVIP

DOI: 10.6023/cjoc201211052 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 水杨酰芳胺类化合物的设计、合成及体外抗肿瘤活性研究 王 杰a 邬 皓a 李家明*,a 许勤龙a 何广卫b 钟国琛a 张艳春a (a 安徽中医学院药学院 安徽省现代中药重点实验室 合肥 230031) (b 合肥医工医药有限公司 合肥 230059) 摘要 根据骨架迁跃原理, 设计并合成了一系列具有酪氨酸激酶抑制剂拉帕替尼(Lapatinib)和诺拉替尼(Neratinib)结构 片段的水杨酰芳胺类化合物, 其结构均经 IR, 1H NMR, 13C NMR 和 MS 确证. 采用四甲基偶氮唑盐(MTT)法考察所合成 化合物的体外抗肿瘤细胞(A549, MCF-7, SGC-7901, Bel-7402)活性. 结果表明, 所合成的化合物对 4 种肿瘤细胞增殖均 有一定的抑制活性, 部分化合物的活性强于阳性对照药吉非替尼(Gefitinib). 关键词 水杨酰芳胺; 酪氨酸激酶抑制剂; 抗肿瘤 Design, Synthesis, and Biological Evaluation of N-Aryl-salicylamide Derivatives as Potential Antitumor Agents Wang, Jiea Wu, Haoa Li, Jiaming*,a Xu, Qinlonga He, Guangweib Zhong, Guochena Zhang, Yanchuna a ( Anhui Key Laboratory of Traditional Chinese Medicine , Department of Pharmacy, Anhui College of Traditional Chinese Medicine , Hefei 230031) b ( Hefei Medical Engineering Pharmaceutical Co, Ltd., Hefei 230059) Abstract According to the scaffold hopping, a series of N-aryl-salicylamide derivatives, which have fragments of tyrosine kinase inhibitors lapatinib and neratinib were designed and synthesized. Their structures were identified by IR, 1H NMR, 13C NMR and MS techniques. The target compounds were tested for cytotoxic activity against four cancer cell lines, including A549, MCF-7, SGC-7901, Bel-7402, by meth