喹喔啉衍生物的设计合成及抗肿瘤活性研究

Design and synthesis of quinoxaline derivatives and their antitumor activities

摘要: 目的设计和合成新型喹喔啉类抗肿瘤药物。方法以4-氯-2-硝基苯胺为起始原料经取代、还原关环、氧化、和氯代合成了中间体2，7-二氯喹喔啉(7)，再在喹喔啉的2位引入不同的取代酚结构单元，合成了一系列共9个新喹喔啉衍生物。结果目标产物利用¹H NMR,MS和IR进行结构确认。结论初步体外抗肿瘤活性测试表明，在1×10^-4 mol·L^-1浓度时，部分目标化合物的抗肿瘤活性和XK469相当。

Abstract: AimTo design and synthesize novel quinoxaline derivatives as antitumor agents. MethodsUsing 4-chloro-2-nitroaniline as a starting compound, followed by substitution, reductive cyclization, oxidation, and chlorination, to give the key intermediate 2,7-dichloroquinoxaline (7), which reacted with different phenolic compounds to afford quinoxaline derivatives. ResultsThe structures of the target molecules were characterized by elemental analysis, ¹H NMR, MS, and IR. ConclusionAt concentration of 1×10^-4 mol·L^-1, some of the derivatives showed equal antitumor activities to XK469.