呋喃氟尿嘧啶衍生物BFT-1的合成及其抗肿瘤活性.pdfVIP

242 食品与药品 Food and Drug 2011年第 13卷第07期 呋喃氟尿嘧啶衍生物BFT-1的合成及其抗肿瘤活性 1 1 2 1 刘爱芹 ，周 玲 ，薛 源 ，于胜海 （1. 山东省医学科学院药物研究所，山东 济南250062 ；2. 山东省医学科学院附属医院，山东 济南 250062 ） 摘 要：目的 探索高效低毒的抗肿瘤药物。方法 替加氟 （FT-207 ）为先导化合物，合成1-( 四氢-2-呋喃基)-3- (2- 甲基苯 甲酰基)-5-氟-2,4( 1H,3H)-嘧啶二酮(BFT- 1) ，并进行抗肿瘤活性筛选。结果 BFT- 1结构经红外光谱、质谱、元素分析和1H- NMR确证，总收率为32.5 % 。初步药理筛选结果显示BFT- 1具有抗肿瘤活性，抑瘤率与FT-207相近，但BFT- 1有效剂量范 围较大，动物体重下降幅度小，耐受性好。结论 BFT-1值得深入研究。 关键词：呋喃氟尿嘧啶衍生物BFT-1；合成；抗肿瘤活性 中图分类号：TQ460.31 文献标识码：A 文章编号：1672-979X （2011）07-0242-03 Synthesis and Antineoplastic Activity of Ftorafur Derivate BFT-1 1 1 2 1 LIU Ai-qin , ZHOU Ling , XUE Yuan , YU Sheng-hai (1.Institute of Materia Medica, Shangdong Academy of Medical Sciences, Jinan 250062, China; 2. Aff iliated Hosp ital of Shangdong Academy of Medical Sciences Jinan 250062, China) Abstract: Objective To obtain an antitumor drug with high antitumor effect and low toxicity. Methods Take ftorafur(FT-207) as the lead compound, the 1-(tetrahydro -2-furyl)-3-(2-methylbenzoyl)-5-fluorine-2,4( 1H,3H)- pyrimidinedione (BFT- 1) were synthesized and screened for the study of their antineoplastic activity. Results The structure of BFT- 1 was identified by IR, MS, elemental analysis and 1H-NMR, the overall yeild was 32.5 %. The preliminary pharmacological test showed that the BFT-1 possesses the antineoplasmic activity with a similar efficiency to that of FT-207. The effective dose of BFT-1 ranged widely. The weight loss of treated animals is slight and the animals were well tolerated. Conclusion BFT-1 deserves further study. Key Words: ftorafur derivate BFT-1; synthesis; antineoplastic activity