Objective: Coupling of ethyl 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)acetate 2 with diazotized anilines in ethanol in the presence of sodium acetate yielded 2-(2-arylhydrazono)-2-(6,7- dimethoxy-3,4-dihydroisoquinolin-1-yl)acetate (4a-f).

Methods: Treatment of 2 with α-bromoketones 6a-f in dry benzene at reflux gave the corresponding isoquinolinium bromides 7a-f. Refluxing of each of the salts 7a-f in dry benzene and in the presence of triethylamine yielded 2-arylpyrrolo-[2,1-a]isoquinoline structures 8a-f, that converted to ethyl (E)-8,9- dimethoxy-3-(phenyldiazen-yl)-2-(aryl)-5,6-dihydropyrrolo[2,1-a]isoquinoline-1-carboxylate (9a-f) upon treatment with diazotized anilines 3 in ethanol in the presence of sodium acetate.

Results and Conclusion: Cytotoxic assay was performed for in vitro antitumor screening against caucasian breast adenocarcinoma (MCF7), hepatocellular carcinoma (HepG2) and colorectal carcinoma (HCT-116) cell lines. The results were compared with the standard anticancer drug (doxorubicin). Molecular docking using MOE 2014.09 software was carried out for the most potent compound 4d, which showed the highest binding affinity towards the four tested proteins and thus initiated apoptosis of cancer cells.

目的：在乙酸钠存在下，将2-（6,7-二甲氧基-3,4-二氢异喹啉-1-基）乙酸乙酯2与重氮化苯胺在乙醇中偶联，得到2-（2-芳基肼基）-2-（6 ，7，7-二甲氧基-3，4-二氢异喹啉-1-基）乙酸酯（4a-f）。

方法：在回流的无水苯中用α-溴酮6a-f处理2，得到相应的溴化异喹啉鎓7a-f。每种盐7a-f在干燥的苯中并在三乙胺的存在下回流，生成2-芳基吡咯并-[2,1-a]异喹啉结构8a-f，该结构转化为乙基（E）-8,9-二甲氧基-在乙酸钠存在下在乙醇中用重氮化苯胺3处理3-（苯基重氮基）-2-（芳基）-5,6-二氢吡咯并[2,1-a]异喹啉-1-羧酸酯（9a-f） 。

结果与结论：进行了细胞毒性试验，以针对白种人乳腺腺癌（MCF7），肝细胞癌（HepG2）和结直肠癌（HCT-116）细胞系进行体外抗肿瘤筛选。将结果与标准抗癌药（阿霉素）进行比较。使用MOE 2014.09软件对最有效的化合物4d进行了分子对接，该化合物对四个被测蛋白显示出最高的结合亲和力，从而启动了癌细胞的凋亡。