Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives

doi:10.6023/cjoc201908012

Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (3): 794-800.DOI: 10.6023/cjoc201908012 Previous Articles Next Articles

新型1,3-二取代酞嗪酮类衍生物的合成及抗肿瘤活性研究

张路野^a,b, 张洋^a,b, 包崇男^a,b, 杨鹏^a,b, 李二冬^a,b, 孟娅琪^a,b, 崔飞^a,b, 周蕊^a,b, 黄诗雨^a,b, 郑甲信^a,b, 单丽红^a,d, 刘宏民^a,b,c,d, 张秋荣^a,b,d

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;
c 省部共建食管癌防治国家重点实验室郑州 450052;
d 教育部药物制备关键技术重点实验室郑州 450001

收稿日期:2019-08-08 修回日期:2019-10-11 发布日期:2020-04-02
通讯作者: 郑甲信, 单丽红, 刘宏民, 张秋荣 E-mail:zqr409@yeah.net;shlh@zzu.edu.cn;liuhm@zzu.edu.cn;zjx1224@163.com
基金资助:
国家自然科学基金（No.81430085）、河南省自然科学基金（No.182300410321）、省部共建食管癌防治国家重点实验室开放基金（No.K2020000X）资助项目.

Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives

Zhang Luye^a,b, Zhang Yang^a,b, Bao Chongnan^a,b, Yang Peng^a,b, Li Erdong^a,b, Meng Yaqi^a,b, Cui Fei^a,b, Zhou Rui^a,b, Huang Shiyu^a,b, Zheng Jiaxin^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, Zhengzhou 450001;
c State Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou University y, Zhengzhou 450052;
d Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education of China, Zhengzhou 450001

Received:2019-08-08 Revised:2019-10-11 Published:2020-04-02
Supported by:
Project supported by the National Natural Science Foundation of China (No. 81430085), the Natural Science Foundation of Henan Province (No. 182300410321), and the Openning Fund from State Key Laboratory of Esophageal Cancer Prevention & Treatment (No. K2020000X).

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Abstract

In order to find more efficient and low toxicity antitumor drugs, a series of novel 1,3-disubstituted pyridazinone derivatives were synthesized and evaluated for their antiproliferative activities against four human cancer cell lines (MCF-7, PC-3, SW-620 and HGC-27) in vitro. The results showed that most compounds had good antiproliferative activities, especially 2-(4-(4-bromophenyl)-1-oxo-tolylazine-2(1H)-yl)-N-(2-fluorophenyl)acetamide (5g) exhibited better antiproliferative activities with IC₅₀ value of 6.01 μmol/L. In a nutshell, this work provided clues to discover antitumor agent based on the quinazoline scaffold.

Key words: pyridazinederiv, ative, synthesis, antiproliferative activity

Cite this article

Zhang Luye, Zhang Yang, Bao Chongnan, Yang Peng, Li Erdong, Meng Yaqi, Cui Fei, Zhou Rui, Huang Shiyu, Zheng Jiaxin, Shan Lihong, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives[J]. Chinese Journal of Organic Chemistry, 2020, 40(3): 794-800.

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新型1,3-二取代酞嗪酮类衍生物的合成及抗肿瘤活性研究

Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives

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