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目的合成吲哚拉新5-氟尿嘧啶甲酯,考察其抗肿瘤活性。方法以5-氟尿嘧啶及吲哚拉新为主要原料经2步反应合成目的化合物。以小鼠肉瘤S180、肝癌H22和Lewis肺癌实体瘤为指标,测定产物的抑瘤率。结果经1H-NMR、MS及IR确证目标产物结构;产物对小鼠肉瘤S180、肝癌H22及Lewis肺癌3种实体瘤的抑制作用与5-氟尿嘧啶相近。结论吲哚拉新5-氟尿嘧啶甲酯为抗癌新药。
Objective To synthesize indolazine 5-fluorouracil methyl ester and study its anti-tumor activity. Methods The target compounds were synthesized via 2 steps using 5-fluorouracil and indolazone as the main raw materials. The inhibition rate of the product was determined by using mouse sarcoma S180, liver cancer H22 and Lewis lung solid tumor as indicators. Results The structure of the target product was confirmed by 1H-NMR, MS and IR. The inhibitory effect of the product on mouse sarcoma S180, hepatoma H22 and Lewis lung carcinoma was similar to that of 5-fluorouracil. Conclusion Indolazine 5-fluorouracil methyl ester is a new anticancer drug.