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

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

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146.43μmol·L^-1).

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).