Design,synthesis,and antitumor activity of 2-anilinoquinoline derivatives
Objective To yield a novel 2-anilinoquinoline derivative by introducing a lipophilic aniline group at the C-2 position of the quinoline ring and a hydrophilic group at the C-7 position,and to explore its anti-tumor cell proliferation activity.Methods Key intermediates were synthesized from DL-phenylalanine,L-phenylalanine,and D-phenylalanine,and a series of 2-anilinoquinoline derivatives were synthesized by linking them with quinoline nuclei.The anti-proliferative activity of the target compound on human liver cancer cells(HepgG2)and non-small cell lung cancer cells(A549)was tested using the CCK-8 method.The binding effects of the target compound with vascular endothelial growth factor receptor(VEGFR)and epidermal growth factor receptor(EGFR)proteins were determined by Autodock software.Results Sixteen new 2-anilinoquinoline derivatives were synthesized,and their structures were confirmed by 1H NMR and LC-MS.The results of in vitro anti-tumor experiments showed that the anti-tumor activities of target compounds T-7 and T-8 were comparable to those of the positive control medicines,Gefitinib and Lenvatinib.The test results of Autodock software were consistent with the results of in vitro anti-tumor experiments.Conclusion The novel 2-anilinoquinoline derivatives have effects against liver cancer and non-small cell lung cancer,laying a theoretical foundation for further exploration of quinoline derivatives as anti-tumor agents.
万方数据
维普
