2-甲硫基-4-芳胺喹唑啉衍生物的合成及抗肿瘤活性评价
收稿日期: 2018-05-04
修回日期: 2018-06-20
网络出版日期: 2018-07-05
基金资助
国家自然科学基金（No.81430085）、河南省科技厅项目（Nos.182300410321，182102310249）和郑州大学大学生创新创业训练计划（No.2017cxcy563）资助项目.
Synthesis and Antitumor Activities Evaluation of 2-Methylthio-4-arylamine Quinazoline Derivatives
Received date: 2018-05-04
Revised date: 2018-06-20
Online 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).
孟祥川 , 栗娜 , 李二冬 , 常通航 , 刘梦 , 柳晴怡 , 袁文娟 , 张晴晴 , 张钰 , 周智玉 , 宋攀攀 , 刘宏民 , 张秋荣 . 2-甲硫基-4-芳胺喹唑啉衍生物的合成及抗肿瘤活性评价[J]. 有机化学, 2018 , 38(11) : 3063 -3069 . DOI: 10.6023/cjoc201805015
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
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