Chinese Journal of Organic Chemistry >
Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives
Received date: 2017-07-22
Revised date: 2017-09-29
Online published: 2017-10-20
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).
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
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
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