Citation: 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]. Chinese Journal of Organic Chemistry, ;2018, 38(11): 3063-3069. doi: 10.6023/cjoc201805015 shu

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

Corresponding author: Liu Hongmin, liuhm@zzu.edu.cn Zhang Qiurong, zqr409@yeah.net
Received Date: 4 May 2018
Revised Date: 20 June 2018
Available Online: 5 November 2018
Fund Project: the Technology Department Project of Henan Province 182300410321Project 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)the National Natural Science Foundation of China 81430085the Students' Platform for Innovation and Entrepreneurship Training Program of Zhengzhou University 2017-cxcy563the Technology Department Project of Henan Province 182102310249

Figures(2)

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.
- quinazoline derivatives,
- synthesis,
- antitumor activity,
- evaluation
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