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以6-氯-5-氰基烟酸、3-氰基-4-氟苯甲酸、4-氰基-3-氟苯甲酸和6-氯-5氰基-2-吡啶甲酸为原料,经过酰胺化和关环两步反应合成了2,4-二氨基喹唑啉和2,4-二氨基吡啶并[2,3-d]嘧啶衍生物,该方法操作简便,除6-氯-5-氰基-2-吡啶甲酸外,其它三种酸的反应收率可达65%以上.采用氢核磁(1H NMR)、碳核磁(13C NMR)和高效液质联用(LC-MS)分析对目标产物进行了表征.采用四甲基偶氮唑盐(MTT)法考察所合成化合物的体外抗肿瘤活性测性,结果表明部分化合物对所选肿瘤细胞的增殖有一定的抑制活性,化合物4c,4d,4e和4f对人白血病细胞(K562)和人肝癌细胞(HepG2)的抑制活性强于阳性对照药5-氟尿嘧啶(5-Fu).
5-cyanonicotinic acid, 3-cyano-4-fluorobenzoic acid, 4-cyano-3-fluorobenzoic acid and 6-chloro-5-cyano-2-pyridinecarboxylic acid as raw materials, 2,4-diamino-quinazoline and 2,4-diaminopyrido [2,3-d] pyrimidine derivatives were synthesized by amidation and ring-closing reaction. The method was simple and convenient. In addition to 6- -cyano-2-pyridinecarboxylic acid, the yields of the other three acids were over 65% .H NMR, 13C NMR and LC-MS The target product was characterized by MTT assay.The in vitro antitumor activity of the synthesized compounds showed that some of the compounds had certain inhibitory activity on the proliferation of selected tumor cells.Compound 4c , 4d, 4e and 4f on human leukemia cells (K562) and human hepatocellular carcinoma cells (HepG2) were stronger than the positive control drug 5-fluorouracil (5-Fu).