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

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1HNMR,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1×10-4mol·L-1浓度时,部分目标化合物的抗肿瘤活性和XK469相当。

Aim To design and synthesize novel quinoxaline derivatives as antitumor agents. Methods Using 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. Results The structures of the target molecules were characterized by elemental analysis, ~I^I NMR, MS, and IR. Conclusion At concentration of 1 × 10^-4 mol · L^-1, some of the derivatives showed equal antitumor activities to XK469.