有机化学 ›› 2016, Vol. 36 ›› Issue (5): 1044-1050.DOI: 10.6023/cjoc201510018 上一篇    下一篇

研究论文

2-取代苯氨基喹唑啉衍生物的合成及抗肿瘤活性研究

潘晓乐, 王磊, 顿艳艳, 方浩   

  1. 山东大学药学院 济南 250012
  • 收稿日期:2015-10-16 修回日期:2016-01-03 出版日期:2016-05-25 发布日期:2016-01-29
  • 通讯作者: 方浩 E-mail:haofangcn@sdu.edu.cn
  • 基金资助:

    国家自然科学基金((No.81373281))资助项目.

Synthesis and Antiproliferative Activity Studies on 2-Substitued Aniline Quinazoline Derivatives

Pan Xiaole, Wang Lei, Dun Yanyan, Fang Hao   

  1. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012
  • Received:2015-10-16 Revised:2016-01-03 Online:2016-05-25 Published:2016-01-29
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81373281).

以2,4-喹唑啉二酮为起始原料,通过氯代、Suzuki偶联和芳环亲核取代反应得到一系列2-取代苯氨基喹唑啉衍生物,并经1H NMR,13C NMR和HRMS进行结构确证.应用溴化噻唑蓝四氮唑(MTT)法对目标化合物进行了初步体外抗肿瘤细胞增殖活性研究.结果表明,部分化合物具有较好的体外抗肿瘤细胞增殖活性,其中活性化合物4u4v对Hela,A549和MCF-7三种肿瘤细胞株的增殖均有明显抑制作用.

关键词: 喹唑啉衍生物, 抗肿瘤活性, 合成

A series of 2-substituted aniline quinazoline derivatives were prepared with the starting material of quinazoline-2,4(1H,3H)-dione, and then followed by the reaction of chlorination, Suzuki reaction and nucleophilic substitution. The structures of target compounds were identified by 1H NMR, 13C NMR and HRMS. The preliminary biological evaluations were performed using thiazolyl blue tetrazolium bromide (MTT) method to test their antiproliferative activities against some tumor cell lines. The results suggest that some compounds have the abilities to inhibit the growth of Hela tumor cell lines, and most potent compounds 4u and 4v alsoexhibit good antiproliferative activities against A549 and MCF-7 tumor cell lines.

Key words: quinazoline derivatives, antitumor activity, synthesis