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以硫醇、硫脲、2-氨基-5-巯基-1,3,4-噻二唑等为原料,通过两步反应合成了10个新的含1,3,4-噻二唑的二硫醚衍生物,并利用IR,~1H NMR,ESI-MS和元素分析对目标化合物进行了结构表征.采用CCK-8法测试了目标产物对人体肝癌细胞SMMC-7721,乳腺癌细胞MCF-7和肺癌细胞A549等肿瘤细胞的增殖抑制活性.结果表明,对于不同的肿瘤细胞,大多数试验化合物显示了较好的增殖抑制活性,且其活性优于阳性对照药5-氟尿嘧啶.尤其是正丙基(2-氨基-1,3,4-噻二唑-5-基)二硫醚(3b)和正丁基(2-氨基-1,3,4-噻二唑-5-基)二硫醚(3d),对SMMC-7721细胞显示了高效的增殖抑制效果,IC50值分别为1.68和1.93μmol/L.4-氯苄基(2-氨基-1,3,4-噻二唑-5-基)二硫醚(3i)对MCF-7细胞表现了显著的抗增殖活性(IC50值为1.78μmol/L),且对A549细胞展现了最好的抑制效果(IC50值为4.04μmol/L).
Thiols, thiourea, 2-amino-5-mercapto-1,3,4-thiadiazole were used as starting materials to synthesize 10 new bis The thioether derivatives were characterized by means of IR, 1H NMR, ESI-MS and elemental analysis.The CCK-8 method was used to test the effect of the target product on human hepatocellular carcinoma cell line SMMC-7721, breast cancer cell line MCF-7 And lung cancer cells A549 and other tumor cells.The results showed that for different tumor cells, most of the test compounds showed good proliferation inhibitory activity, and its activity is superior to the positive control drug 5-fluorouracil, especially n-propyl (2-amino-1,3,4-thiadiazol-5-yl) disulfide (3b) and n-butyl (3d) showed high proliferation inhibitory effect on SMMC-7721 cells with IC50 values of 1.68 and 1.93 μmol / L, respectively. 4-Chlorobenzyl (2-amino- (3i) showed significant anti-proliferative activity (IC50 = 1.78μmol / L) on MCF-7 cells and showed the best inhibitory effect on A549 cells (IC50 = 4.04μmol / L) .