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有机化学 ›› 2019, Vol. 39 ›› Issue (11): 3283-3288.DOI: 10.6023/cjoc201905035 上一篇    下一篇

研究简报

1, 3, 4-噻二唑三氮烯酰胺衍生物的合成及抗肿瘤活性研究

陈彦君a, 张明千b, 李子秋b, 罗德福b, 李龙辉b, 俞婷婷c, 龙跃b*()   

  1. a焦作大学化学与环境工程学院 河南焦作 454003
    b 郑州大学化学与分子工程学院 郑州 450001
    c 郑州大学药学院 郑州 450001
  • 收稿日期:2019-05-14 发布日期:2019-07-17
  • 通讯作者: 龙跃 E-mail:longyue@zzu.edu.cn
  • 基金资助:
    国家自然科学基金(J1210060);河南省科技攻关计划(0624420031);河南省基础研究基金(022463001)

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

Chen Yanjuna, Zhang Mingqianb, Li Ziqiub, Luo Defub, Li Longhuib, Yu Tingtingc, Long Yueb*()   

  1. 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
  • Received:2019-05-14 Published:2019-07-17
  • Contact: Long Yue E-mail:longyue@zzu.edu.cn
  • Supported by:
    the National Natural Science Foundation of China(J1210060);the Science and Technology Planning Project of Henan Province(0624420031);the Basic Research Development Program of Henan Province(022463001)

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把三氮烯结构与1，3，4-噻二唑、酰胺相拼接，合成了14个未见报道的1，3，4-噻二唑三氮烯酰胺衍生物，并用核磁共振谱（NMR）、红外光谱（IR）和高分辨质谱（HRMS）等方法对化合物结构进行表征.通过以典型三氮烯药物达卡巴嗪作参照，对人食管癌细胞（EC109）、人胃癌细胞（MGC803）和人前列腺癌细胞（PC-3）做活性检测，结果显示化合物8a，8h，8i，8k，8l对人前列腺癌细胞（PC-3）的抑制活性最好，其IC50值分别为33.02，34.05，7.71，4.82，23.84μmol·L-1，远低于对照药达卡巴嗪（IC50值为146.43 μmol·L-1）.

关键词: 三氮烯, 1, 3, 4-噻二唑, 酰胺, 人食管癌细胞, 人胃癌细胞, 人前列腺癌细胞

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).

Key words: triazene, ?, amide, human esophageal cancer cells, human gastric cancer cells, human prostate cancer cells