N_1-(芳)烷酰氧亚甲基-5-氟尿嘧啶的合成及其初步抗肿瘤活性的研究  

Study on the synthesis and antitumor activity of N_1-(aryl)alkyl acyloxymethyl-5-fluorouracil derivatives

作　　者：蒋庆琳[1] 吴林艳[1] 吴勇[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2005年第1期12-14,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目 (批准号 :3 9970 869)

摘　　要：目的　合成抗肿瘤活性高 ,毒性小的N1- (芳 )烷酰氧亚甲基取代的 5 -氟尿嘧啶衍生物。方法　以 5 -氟尿嘧啶为原料 ,经与甲醛加成反应后 ,和二酸单苄酯反应即得目标物 3a、3b、3c ,并采用MTT法及SRB法评价目标物 3的抗肿瘤活性。结果　合成了 3个目标物 3a、3b、3c ,其结构经1HNMR、IR和MS确证。结论　体外抗肿瘤活性筛选结果显示 3b和 3c有较强的抗肿瘤活性。OBJECTIVE To synthesize N 1-(aryl)alkylacyloxymethyl-5-fluorouracil derivatives which has higher antitumor activities and less toxicities.METHODS Title compounds 3a, 3b, 3c were prepared with the starting material 5-fluorouracil, which was added by formalin and then coupled with monobenzyl dicarboxylates.Their bioactivities were evaluated by MTT and SRB methods. RESULTS Three title compounds 3a,3b,3c were synthesized which had been confirmed by IR, 1HNMR and MS. CONCLUSION 3b and 3c could strongly inhibit the proliferation of tumor cells in vitro.

关 键 词：5-氟尿嘧啶 体外抗肿瘤活性 MS SRB法 毒性 IR 反应 合成 亚甲基 取代 

分 类 号：R979.1[医药卫生—药品] R730[医药卫生—药学]