【摘要】 目的 发现高效、低毒的新型抗肿瘤目标化合物。方法 以4-甲氧基苯胺为原料，通过氨解、环化、氯代、偶联、烷基化等反应，设计并合成一系列新型4-三氟甲基-6-甲氧基喹啉-2-胺衍生物，并通过¹H NMR、¹³C NMR、¹⁹F NMR进行结构确证。采用MTT法评价目标化合物对K562细胞（人慢性髓系白血病细胞）、LNCaP细胞（前列腺癌细胞）、PC3细胞（前列腺癌细胞）、HeLa细胞（人宫颈癌细胞）和A549细胞（人肺癌细胞）5种肿瘤细胞株的生长抑制活性。结果 共合成了4-三氟甲基-6-甲氧基喹啉-2-胺衍生物17个。其中，在5μmol·L^-1浓度下，化合物5b对LNCaP细胞抑制率为42.61%，化合物5e对K562细胞抑制率为41.29%。结论 建立了一种新型4-三氟甲基-6-甲氧基喹啉-2-胺衍生物的快速合成方法，部分化合物对肿瘤细胞的增殖具有一定的抑制活性，可为该类化合物的深入研究提供参考。更多还原

【Abstract】 Objective To discover new antitumor target compounds with high efficiency and low toxicity.Methods A series of novel 6-methoxy-4-trifluoromethyl-quinolin-2-amine derivatives were designed and synthesized starting with 4-methoxaniline through amination,cyclization,chlorination,coupling,and alkylation reactions.The structures of all target compounds were characterized by ¹H NMR,¹³C NMR,and ¹⁹F NMR.The antiproliferation activities of the target compounds on tumor cell lines （such as K562,LNCaP,PC3,HeLa,and A549） in vitro were evaluated by MTT assay.Results Totally 17 6-methoxy-4-trifluoromethyl-quinolin-2-amine derivatives were synthesized.At a concentration of 5μmol·L^-1,the inhibitory rate of compound 5b on LNCaP cells was 42.61%,and the inhibitory rate of compound 5e on K562 cells was 41.29%.Conclusion The method for novel6-methoxy-4-trifluoromethyl-quinolin-2-amine derivatives has been established,and some of the target compounds exhibit certain inhibition on the proliferation of tumor cells.This study provides a basis for further research on the derivatives of 6-methoxy-4-trifluoromethyl-quinolin-2-amine.更多还原