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[目的]合成5,6,7,8-四氢-[1,2,4]三唑并[5,1-b]喹唑啉衍生物,并观察其抗肿瘤作用.[方法]环己酮-2-羧酸甲酯与3-氨基-1,2,4-三唑缩合反应生成5,6,7,8-四氢-[1,2,4]三唑并[5,1-b]喹唑啉-9-醇,然后进行氯代反应得到中间体2,最后烷基化得到新型9-取代-5,6,7,8-四氢-[1,2,4]三唑并[5,1-b]喹唑啉化合物(3a~3n).化合物结构均经1 H-NMR,IR,MS确认.采用MTT比色法进行化合物抑制人体Bel-7402肝癌细胞、HCT-8结肠癌细胞及A549肺癌细胞体外活性测试.[结果]部分化合物对人体Bel-7402肝癌细胞、HCT-8结肠癌细胞及A549肺癌细胞表现出不同程度的抑制作用.其中化合物3h在5mg/L质量浓度下对A549肺癌细胞的抑制率达到82.00%.[结论]5,6,7,8-四氢-[1,2,4]三唑并[5,1-b]喹唑啉衍生物对人体肿瘤细胞表现出不同程度的抑制作用,其中化合物3h的抑制率最高.
[Objective] To synthesize 5,6,7,8-tetrahydro- [1,2,4] triazolo [5,1-b] quinazoline derivatives and observe their antitumor effect. [Method] Ketone-2-carboxylic acid methyl ester was condensed with 3-amino-1,2,4-triazole to give 5,6,7,8-tetrahydro- [1,2,4] triazolo [5,1- b] quinazolin-9-ol, followed by chlorination to give Intermediate 2 and finally alkylated to give the novel 9-substituted-5,6,7,8-tetrahydro- [1,2,4] triazole The structures of the compounds were confirmed by 1 H-NMR, IR and MS. The compounds were used to inhibit the growth of Bel-7402 hepatocarcinoma cells, HCT-8 Colon cancer cells and A549 lung cancer cells in vitro. [Results] Some compounds showed inhibitory effects on human Bel-7402 hepatocarcinoma cells, HCT-8 colon carcinoma cells and A549 lung cancer cells to varying degrees. Among them, The inhibitory rate of A549 cells was 82.00%. [Conclusion] The inhibitory effect of 5,6,7,8-tetrahydro- [1,2,4] triazolo [5,1-b] quinazoline derivatives on Human tumor cells showed different degrees of inhibition, of which compound 3h the highest inhibition rate.