Citation: Chen Yanjun, Zhang Mingqian, Li Ziqiu, Luo Defu, Li Longhui, Yu Tingting, Long Yue. Synthesis and Antitumor Activities of 1, 3, 4-Thiadiazole Triazene Amide Derivatives[J]. Chinese Journal of Organic Chemistry, ;2019, 39(11): 3283-3288. doi: 10.6023/cjoc201905035 shu

Synthesis and Antitumor Activities of 1, 3, 4-Thiadiazole Triazene Amide Derivatives

Chen Yanjun ^a ,
Zhang Mingqian ^b ,
Li Ziqiu ^b ,
Luo Defu ^b ,
Li Longhui ^b ,
Yu Tingting ^c ,
Long Yue ^b,,

a.
Department of Chemical and Environmental Engineering, Jiaozuo Universiy, Jiaozuo, Henan 454003
b.
College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001
c.
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001

Corresponding author: Long Yue, longyue@zzu.edu.cn
Received Date: 14 May 2019
Revised Date: 18 June 2019
Available Online: 17 November 2019
Fund Project: Project supported by the National Natural Science Foundation of China (No. J1210060), the Science and Technology Planning Project of Henan Province (No. 0624420031) and the Basic Research Development Program of Henan Province (No. 022463001)the Science and Technology Planning Project of Henan Province 0624420031the Basic Research Development Program of Henan Province 022463001the National Natural Science Foundation of China J1210060

Figures(2)

By splicing the triazene structure with 1, 3, 4-thiadiazole and amide, fourteen unreported 1, 3, 4-thiadiazole triazene amide derivatives were synthesized. The structures of these compounds were characterized by nuclear magnetic resonance (NMR), infrared spectroscopy (IR) and high-resolution mass spectrometry (HRMS). By using the typical triazene drug dacarbazine as a reference, the activity detections of human esophageal cancer cells (EC109), human gastric cancer cells (MGC803) and human prostate cancer cells (PC-3) were carried out. The results showed that compounds 8a, 8h, 8i, 8k, and 8l had the best inhibitory activity against human prostate cancer cells (PC-3). And their IC₅₀ values were 33.02, 34.05, 7.71, 4.82, 23.84 μmol·L^-1, which were far lower than the control drug their IC₅₀ values were 33.02, 34.05, 7.71, 4.82, 23.84 μmol·L^-1, which were far lower than the control drug dacarbazine (146.43 μmol·L^-1).
- triazene,
- ,
- amide,
- human esophageal cancer cells,
- human gastric cancer cells,
- human prostate cancer cells
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