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目的:设计合成一系列4-取代-7-氯喹啉衍生物并测定其抗肿瘤活性。方法:4,7-二氯喹啉通过烃化反应及缩合反应得到目标化合物,并采用MTT法,评价了其对4种体外培养肿瘤细胞的生长抑制作用。结果:大多数化合物具有一定的抑制肿瘤细胞增殖的活性,其中化合物3,5和10a抑制人非小细胞肺癌A549,NCI-H446,Hela细胞生长的作用强于阳性对照,化合物5和10a对于人非小细胞肺癌A549的抑制活性是阳性对照药的4~5倍,明显优于阳性对照。结论:本文合成的该系列部分化合物具有较好的抗肿瘤活性,是潜在的抗肿瘤候选药物。
AIM: To design and synthesize a series of 4-substituted 7-chloroquinoline derivatives and determine their anti-tumor activity. Methods: 4,7-Dichloroquinoline was synthesized by the reaction of alkylation and condensation. The inhibitory effect of 4,7-dichloroquinoline on the growth of 4 tumor cells was evaluated by MTT assay. Results: Most of the compounds had certain activity of inhibiting the proliferation of tumor cells. Compounds 3, 5 and 10a inhibited the growth of human non-small cell lung cancer A549, NCI-H446 and Hela cell more than the positive control, The inhibitory activity of non-small cell lung cancer A549 is 4-5 times that of the positive control drug, which is obviously better than the positive control. Conclusion: Some of the compounds synthesized in this paper have good anti-tumor activity and are potential anticancer drugs.