Objective To synthesize and evaluate novel and potent prodrugs of 5-fluorouracil (5-Fu).Methods Six prodrugs of 5-Fu were prepared by incorporated various substituents on N 1 and N 3 position.The in vitro antiproliferative activity against five cancer cell lines was evaluated by MTT assay.Results All the six prodrugs of 5-Fu displayed potent antiproliferative activity against canc-er cell lines.Conclusion These novel prodrugs exhibited potent anticancer activity,and were worth of further investigation.%目的：寻找新型、高效的5-氟尿嘧啶(5-Fu)前药并测定其抗肿瘤活性。方法在5-氟尿嘧啶的 N 1和 N 3位引入具有抗肿瘤活性的取代基，合成其前体药物，利用 MTT 方法测定其对不同肿瘤细胞的增殖抑制活性。结果合成的6个5-氟尿嘧啶前体药物均显示了较好的肿瘤细胞增殖抑制活性。结论新型5-氟尿嘧啶前药对肿瘤细胞有较好的抑制活性，值得进一步研究。
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