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以4,5-二甲氧基-2-氨基苯甲酸和醋酸甲眯为起始原料,经环化、氯化、取代和缩合四步反应,设计、合成了六个未见文献报道的含有缩氨基硫脲的喹唑啉衍生物4a～4f,其结构用1H NMR,13C NMR,ESI-MS,IR及元素分析测试技术进行了表征.采用MTT法测试了化合物4a～4f对人胃癌SGC-7901、人口腔表皮样癌KB和人纤维肉瘤HT-1080的体外抗肿瘤活性.初步的测试结果表明,化合物4a和4f对HT1080表现出显著的抗肿瘤活性.
To four 4,5-dimethoxy-2-aminobenzoic acid and methyl acetate as the starting material, cyclization, chlorination, substitution and condensation four-step reaction, design and synthesis of six unreported containing The structure of quinazoline derivatives 4a ~ 4f of thiosemicarbazone was characterized by 1H NMR, 13C NMR, ESI-MS, IR and elemental analysis.MTT assay was used to evaluate the inhibitory effect of compounds 4a ~ 4f on human gastric cancer SGC -7901 in human oral epidermoid carcinoma KB and human fibrosarcoma HT-1080 in vitro.The preliminary test results show that compounds 4a and 4f show significant anti-tumor activity on HT1080.