Design,synthesis and anti-tumoractivity of novel amidine derivatives of doxifluridine  

作　　者：Feng, Ji Lu Sun, Hai Ling Geng, Dong Ping Li, Ke 

机构地区：[1]Second Mil Med Univ, Sch Pharm, Dept Med Chem, Shanghai 200433, Peoples R China

出　　处：《Chinese Chemical Letters》2010年第2期163-166,共4页中国化学快报（英文版）

摘　　要：A series of novel amidine derivatives of doxifluridine were synthesized using acid amide as the starting material,and their antitumor activity was evaluated in A549 cells.Compounds 10 and 11 demonstrated were more potent than 5-Fu,which was used as a positive control.Compound 10,which were found to be the most potent one with IC_(50) of 3.2μmol/L,was 16 times more potent than 5-Fu with IC_(50) of 52μmol/L to the A549 cells.A new route was designed to synthesize 5 -deoxy-5-fluorocytidine.All compounds were c...A series of novel amidine derivatives of doxifluridine were synthesized using acid amide as the starting material,and their antitumor activity was evaluated in A549 cells.Compounds 10 and 11 demonstrated were more potent than 5-Fu,which was used as a positive control.Compound 10,which were found to be the most potent one with IC_(50) of 3.2μmol/L,was 16 times more potent than 5-Fu with IC_(50) of 52μmol/L to the A549 cells.A new route was designed to synthesize 5 -deoxy-5-fluorocytidine.All compounds were c...

关 键 词：Doxifluridine AMIDINE SYNTHESIS ANTI-TUMOR Crystal structure 

分 类 号：O621.3[理学—有机化学]