Citation: Zhang Luye, Zhang Yang, Wang Zhengjie, Wang Tao, Li Erdong, Liu Limin, Liu Xiujuan, Zheng Jiaxin, Ke Yu, Shan Lihong, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Activity of Novel Quinazoline Derivatives Containing Acrylamide[J]. Chinese Journal of Organic Chemistry, ;2020, 40(9): 2804-2810. doi: 10.6023/cjoc202005081 shu

Synthesis and Antitumor Activity of Novel Quinazoline Derivatives Containing Acrylamide

Zhang Luye ^a,b ,
Zhang Yang ^a,b ,
Wang Zhengjie ^a,b ,
Wang Tao ^a,b ,
Li Erdong ^a,b ,
Liu Limin ^a,b ,
Liu Xiujuan ^a,b ,
Zheng Jiaxin ^a,b ,
Ke Yu ^a,b ,
Shan Lihong ^a,d,, ,
Liu Hongmin ^a,b,c,d,, ,
Zhang Qiurong ^a,b,d,,

a.
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
b.
Collaborative Innovation Center of New Drug Research and Safety Evaluation of Henan Province, Zhengzhou 450001
c.
State Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou 450052
d.
Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou 450001

Corresponding author: Shan Lihong, shlh@zzu.edu.cn Liu Hongmin, liuhm@zzu.edu.cn Zhang Qiurong, zqr409@yeah.net
Received Date: 28 May 2020
Revised Date: 17 June 2020
Available Online: 30 June 2020
Fund Project: the National Natural Science Foundation of China U1904163Project supported by the National Natural Science Foundation of China (No. U1904163), and the Opening Fund from State Key Laboratory of Esophageal Cancer Prevention & Treatment (No. K2020000X)the Opening Fund from State Key Laboratory of Esophageal Cancer Prevention & Treatment K2020000X

Figures(2)

In order to find efficient and low toxicity anti-tumor drugs, a series of novel quinazoline derivatives containing N-(3-aminophenyl)acrylamide were synthesized and their antiproliferative activities were evaluated against three human cancer cell lines (H1975, PC-3, MGC-803) by using methyl thiazolyl tetrazolium (MTT) assay. The results showed that most compounds exhibited better antiproliferative activities against the four human tumor cell lines. Among them, N-(3-(2-((4-((4-chlorophenyl)amino)-7-methoxy-quinazolin-6-yl)oxy)acetamido)phenyl)acrylamide (13j) showed the best antiproliferative activity against H1975 and MGC-803 cancer cell lines with IC₅₀ values of (6.77±0.65) and (4.06±0.34) μmol/L, respectively. Its activity was better than the positive control gefitinib. In a nutshell, this work provides clues to discover antitumor agent based on the quinazoline scaffold.
- acrylamide,
- quinazoline,
- synthesis,
- antiproliferative activity
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