Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives

doi:10.6023/cjoc201707025

Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (2): 451-456.DOI: 10.6023/cjoc201707025 Previous Articles Next Articles

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1-苯基-4-取代酞嗪衍生物合成及抗肿瘤活性评价

辛景超^a,b, 栗娜^a,b, 马启胜^a,b, 李二冬^a,b, 孟祥川^a,b, 可钰^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:2017-07-22 修回日期:2017-09-29 发布日期:2017-10-20
通讯作者: 可钰, 刘宏民, 张秋荣 E-mail:ky@zzu.edu.cn;zqr406@sina.com;liuhm@zzu.edu.cn
基金资助:
国家自然科学基金（No.81430085）和郑州市科技局科研（No.141PQYJS554）资助项目.

Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives

Xin Jingchao^a,b, Li Na^a,b, Ma Qisheng^a,b, Li Erdong^a,b, Meng Xiangchuan^a,b, Ke Yu^a,b, Liu Hongmin^a,b, Zhang Qiurong^a,b

a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
b Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001

Received:2017-07-22 Revised:2017-09-29 Published:2017-10-20
Contact: 10.6023/cjoc201707025 E-mail:ky@zzu.edu.cn;zqr406@sina.com;liuhm@zzu.edu.cn
Supported by:
Project supported by the National Natural Science Foundation of China (No. 81430085) and the Research Project of Science and Technology Bureau of Zhengzhou City (No. 141PQYJS554).

1. Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives.PDF(2078KB)

Abstract

In order to find more efficient and economical antitumor drugs, a series of 1-phenyl-4-substituted phthalazine derivatives were synthesized and evaluated for antiproliferative activity in vivo. The structures of the synthesized compounds were confirmed by ¹H NMR, ¹³C NMR and HRMS. The antitumor activity of the target compounds was performed against four cancer cell lines by 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-2-H-tetrazolium bromide (MTT). The results showed that some compounds had a good antitumor activity, especially, N-(4-methoxyphenyl)-2-((4-phenylphthalazin-1-yl) thio) acetamide (5f) and N-(3-chloro-4-fluorophenyl)-2-(4-(4-phenylphthalazin-1-yl) piperazin-1-yl) acetamide (8c), exhibited better antitumor activities with IC₅₀ values of 8.13 and 9.31 μmol•L^-1 against the human esophageal cancer cells, which were superior to 5-fuorouracil.

Key words: synthesis, phthalazine derivative, antitumor activity

Cite this article

Xin Jingchao, Li Na, Ma Qisheng, Li Erdong, Meng Xiangchuan, Ke Yu, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives[J]. Chin. J. Org. Chem., 2018, 38(2): 451-456.

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1-苯基-4-取代酞嗪衍生物合成及抗肿瘤活性评价

Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives

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