Chinese Chemical Letters

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

JL Feng, HL Sun, DP Geng, K Li

Index: Feng, Ji Lu; Sun, Hai Ling; Geng, Dong Ping; Li, Ke Chinese Chemical Letters, 2010 , vol. 21, # 2 p. 163 - 166

Full Text: HTML

Citation Number: 1

Abstract

A series of novel amidine derivatives of doxifluridine were synthesized using acid amide as the starting material, and their anti-tumor 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 IC50 of 3.2 μmol/L, was 16 times more potent than 5-Fu with IC50 of 52μM to the A549 cells. A new route was ...