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

doi:10.6023/cjoc201805015

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

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2-甲硫基-4-芳胺喹唑啉衍生物的合成及抗肿瘤活性评价

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

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 E-mail:liuhm@zzu.edu.cn;zqr409@yeah.net
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

Meng Xiangchuan^a, Li Na^a,b, Li Erdong^a,b, Chang Tonghang^a, Liu Meng^a, Liu Qingyi^a, Yuan Wenjuan^a, Zhang Qingqing^a, Zhang Yu^a, Zhou Zhiyu^a, Song Panpan^a,b, Liu Hongmin^a,b, Zhang Qiurong^a,b

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).

1. Synthesis and Antitumor Activities Evaluation of 2-Methylthio-4-arylamine Quinazoline Derivatives.PDF(8640KB)

Abstract

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

Cite this article

Meng Xiangchuan, Li Na, Li Erdong, Chang Tonghang, Liu Meng, Liu Qingyi, Yuan Wenjuan, Zhang Qingqing, Zhang Yu, Zhou Zhiyu, Song Panpan, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Activities Evaluation of 2-Methylthio-4-arylamine Quinazoline Derivatives[J]. Chin. J. Org. Chem., 2018, 38(11): 3063-3069.

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2-甲硫基-4-芳胺喹唑啉衍生物的合成及抗肿瘤活性评价

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

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