Citation: Ji Lu Feng, Hai Ling Sun, Dong Ping Geng, Ke Li. Design,synthesis and anti-tumoractivity of novel amidine derivatives of doxifluridine[J]. Chinese Chemical Letters, ;2010, 21(2): 163-166. doi: 10.1016/j.cclet.2009.10.013 shu

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

Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received Date: 18 June 2009

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 IC₅₀ of 3.2 μmol/L,was 16 times more potent than 5-Fu with IC₅₀ of 52 μmol/L to the A549 cells.A new route was designed to synthesize 5'-deoxy-5-fluorocytidine.All compounds were characterized by ¹H NMR,MS and X-ray spectras in detail.
- Doxifluridine,
- Amidine,
- Synthesis,
- Anti-tumor,
- Crystal structure
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