Jingchao Xin, Xiangchuan Meng, Hongmin Liu
2018
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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 1 H NMR, 13 C 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 IC 50 values of 8.13 and 9.31 μ mol•L - 1 against the human esophageal cancer cells, which were superior to 5-fuorouracil.