Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (11): 3063-3069.DOI: 10.6023/cjoc201805015 Previous Articles     Next Articles



孟祥川a, 栗娜a,b, 李二冬a,b, 常通航a, 刘梦a, 柳晴怡a, 袁文娟a, 张晴晴a, 张钰a, 周智玉a, 宋攀攀a,b, 刘宏民a,b, 张秋荣a,b   

  1. a 郑州大学药学院 郑州 450001;
    b 新药创制与药物安全性评价河南省协同创新中心 郑州 450001
  • 收稿日期:2018-05-04 修回日期:2018-06-20 发布日期:2018-07-05
  • 通讯作者: 刘宏民, 张秋荣;
  • 基金资助:


Synthesis and Antitumor Activities Evaluation of 2-Methylthio-4-arylamine Quinazoline Derivatives

Meng Xiangchuana, Li Naa,b, Li Erdonga,b, Chang Tonghanga, Liu Menga, Liu Qingyia, Yuan Wenjuana, Zhang Qingqinga, Zhang Yua, Zhou Zhiyua, Song Panpana,b, Liu Hongmina,b, Zhang Qiuronga,b   

  1. a School of Pharmaceutical Science, Zhengzhou University, Zhengzhou 450001;
    b Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001
  • Received:2018-05-04 Revised:2018-06-20 Published:2018-07-05
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81430085), the Technology Department Project of Henan Province (Nos. 182300410321, 182102310249) and the Students' Platform for Innovation and Entrepreneurship Training Program of Zhengzhou University (No. 2017-cxcy563).

In order to find the efficient and novel antitumor drugs, a series of 2-methylthio-4-arylamine quinazoline derivatives were designed and synthesized. The target compounds were evaluated for antitumor activity in vitro on four human cancer cell lines initially including MGC-803, PC-3, HGC-27 and A549. The results showed that some compounds had good antitumor activities, especially N-(4-fluorophenyl)-2-(methylthio) quinazolin-4-amine (9c) and 2-(methylthio)-N-(p-tolyl)-quina-zolin-4-amine (9m), with IC50 values of 0.18 and 0.68 μmol·L-1, respectively.

Key words: quinazoline derivatives, synthesis, antitumor activity, evaluation