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对苯二甲羧酸酯化、肼解、成盐、环化成双-(4-氨基-5-巯基-1,2,4-三唑-3-基)苯(1),再与芳香羧酸(2a~2h)在相转移催化剂四丁基碘化铵和POCl3作用下,高产率制得8种1,4-双[(6-芳基)-1,2,4-三唑并[3,4-b]-[1,3,4]噻二唑-3-基]苯类衍生物(3a~3h),并利用IR、1H NMR、MS和元素分析对目标化合物的结构进行了表征.用MTT方法评价了它们在体外对HepG-2、A549-1和231-2癌细胞株的体外生长抑制活性.结果表明,所合成的8个新化合物均具有潜在的体外抑制癌细胞生长活性,其中3a、3g与3h活性最强.
Terephthalic acid esterification, hydrazinolysis, salt formation, cyclization into bis- (4-amino-5-mercapto-1,2,4-triazol-3-yl) benzene (2a ~ 2h) Under the action of phase transfer catalyst tetrabutylammonium iodide and POCl3, 8 kinds of 1,4-bis [(6-aryl) -1,2,4-triazolo [ 3,4-b] - [1,3,4] thiadiazol-3-yl] benzene derivatives (3a ~ 3h) were synthesized and the structures of the target compounds were characterized by IR, 1H NMR, MS and elemental analysis MTT assay was used to evaluate their in vitro growth inhibitory activity against HepG-2, A549-1 and 231-2 cancer cell lines.The results showed that all of the eight new compounds have the potential to inhibit the growth of cancer cells in vitro Activity, of which 3a, 3g and 3h the strongest activity.