以L-色氨酸和4-氯苯甲醛为原料,经过Pictet-Spengler缩合和氧化脱羧两步反应得到1-(4-氯苯基)-β-咔啉,再经过N9-烷基化和N2-烷基化反应得到12个新的1-(4-氯苯基)-β-咔啉衍生物。目标化合物的结构经1H NMR、元素分析和MS鉴定。采用MTT法考察其对肿瘤细胞的抑制作用,实验结果表明β-咔啉环的N2-烷基化能明显提高抗肿瘤效果,是该类化合物的主要活性位点。 With L-tryptophan and 4-chlorobenzaldehyde as raw materials, Pictet-Spengler condensation and oxidative decarboxylation gave 1- (4-chlorophenyl) -β-carboline and then N9-alkylation and N2-alkylation gives 12 new 1- (4-chlorophenyl) -β-carboline derivatives. The structure of the target compound was confirmed by 1H NMR, elemental analysis and MS. The MTT method was used to investigate its inhibitory effect on tumor cells. The experimental results showed that the N2-alkylation of β-carboline ring can significantly improve the anti-tumor effect, which is the main active site of these compounds.