摘要/Abstract

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


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