Citation: 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]. Chinese Journal of Organic Chemistry, ;2018, 38(2): 451-456. doi: 10.6023/cjoc201707025 shu

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

Corresponding author: Ke Yu, ky@zzu.edu.cn Liu Hongmin, zqr406@sina.com Zhang Qiurong, liuhm@zzu.edu.cn
Received Date: 22 July 2017
Revised Date: 29 September 2017
Available Online: 20 February 2017
Fund Project: 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)the Research Project of Science and Technology Bureau of Zhengzhou City 141PQYJS554the National Natural Science Foundation of China 81430085

Figures(2)

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.
- synthesis,
- phthalazine derivative,
- antitumor activity
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