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 pot...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...展开更多
文摘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...
