吲哚拉新5-氟尿嘧啶甲酯前体药物的制备及其抗肿瘤活性  

Synthesis and antitumor activity of indolacin 5-fluorouracil-1-ylmethyl ester

作　　者：王晶[1] 王岩[1] 卢方正[1] 

机构地区：[1]沈阳药科大学药学院

出　　处：《中国药剂学杂志（网络版）》2012年第3期45-49,共5页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：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 prepare indolacin 5-fluorouracil-1-ylmethyl ester(ILFM) and evaluate its antitumor activity in vivo.Methods The target compound was synthesized by two steps with 5-fluorouracil(5-FU) and indolacin(ILN) as starting materials.S180 sarcoma 、 H22 hapatitic cancer and Lewis-transplanted mice were used to estimate the antitumor activity of indolacin 5-fluorouracil-1-ylmethyl ester compared to 5-FU in vivo.Results The structure of ILFM was confirmed by IR,1H-NMR and MS;and the yield was 73%.The tumor inhibitory rates of ILFM were comparable to that of 5-FU.Conclusion ILFM is a new anticancer drug.

关 键 词：药剂学 前体药物 合成 吲哚拉新5-氟尿嘧啶甲酯 5-氟尿嘧啶 吲哚拉新 抗肿瘤活性 

分 类 号：R943[医药卫生—药剂学] R96[医药卫生—药学]