四氢异喹啉类化合物的设计合成与体外抗肿瘤活性研究

Design,synthesis and in vitro anti-tumor activity of tetrahydroisoquinoline compounds

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,^(13)C-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。

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.