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目的设计和合成苯酰胺类c-Met激酶抑制剂,并测定其体外抗肿瘤活性。方法以4-氯-6,7二甲氧基喹啉、6-氯-7-氮杂嘌呤和4-氯-7-氮杂吲哚为起始物,经取代、还原和缩合反应制备目标化合物3a~5c,并采用噻唑蓝法(MTT)测定目标化合物对GTL-16细胞的抑制作用。结果合成了9个化合物,其结构经MS、1H-NMR和13C-NMR确证。化合物3a~5c对GTL-16细胞均呈现不同程度的抑制作用,其中化合物3c对GTL-16细胞的IC50达到411 nmol/L。结论苯酰胺类化合物具有抑制GTL-16细胞活性的作用,值得进一步深入研究。
Objective To design and synthesize benzamide c-Met kinase inhibitor and determine its anti-tumor activity in vitro. Methods Starting from 4-chloro-6,7-dimethoxyquinoline, 6-chloro-7-azapurine and 4-chloro-7-azaindole, the target was prepared through the substitution, reduction and condensation reactions Compounds 3a ~ 5c, and the inhibitory effect of the target compound on GTL-16 cells was determined by MTT method. Results Nine compounds were synthesized and their structures were confirmed by MS, 1H-NMR and 13C-NMR. Compounds 3a-5c showed different degrees of inhibition on GTL-16 cells, and the IC50 of compound 3c to GTL-16 cells reached 411 nmol / L. Conclusion Benzoamides inhibit the activity of GTL-16 cells and deserve further study.