四氢异喹啉类化合物的设计合成与体外抗肿瘤活性研究

摘要

Objective:To synthesize a series of new tetrahydroisoquinoline compounds and evaluate their anti-tumor activity.Methods:Twelve novel tetrahydroisoquinoline compounds were synthesized by utilizing 3,4-dimethoxyphenethylamine,a series of benzoic acid derivatives and cinnamic acid derivatives as starting materials,subsequently undergoing Bischler-Napieralski reaction,acylation,cyclization,reduction,and hydrolysis.In vitro anti-tumor activities were assessed with SRB reduction assay.Results:The structures of target compounds were characterized by MS,IR,1H NMR and 13C NMR.The results of in vitro anti-tumor activities showed that compound 9e exhibited potential inhibition on HT-29 tumor cell line,and 9f possessed moderate inhibition on HT-29 and HUVEC tumor cell lines.Conclusion:The novel tetrahydroisoquinoline compounds provide a possibility for further investigation.%目的:合成新型四氢异喹啉类化合物,并研究其抗肿瘤活性.方法:以3,4-二甲氧基苯乙胺、一系列苯甲酸衍生物和肉桂酸衍生物为原料,用Bischler-Napieralski反应,经酰化、环合、还原、水解等步骤,得到12个四氢异喹啉类化合物.采用SRB法检测目标化合物的体外抗肿瘤活性.结果:目标化合物结构经MS,1H-NMR,13C-NMR和IR确证.体外抗肿瘤结果显示,化合物9e对HT-29肿瘤细胞株有一定抑制率,化合物9f对HUVEC和HT-29肿瘤细胞株有一定抑制率.结论:该新型四氢异喹啉类具有抑制肿瘤细胞株活性,值得深入研究.