引用本文:
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
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
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
Design,synthesis and anti-tumoractivity of novel amidine derivatives of doxifluridine
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 IC50 of 3.2μmol/L,was 16 times more potent than 5-Fu with IC50 of 52μmol/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.
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关键词:
- Doxifluridine
- / Amidine
- / Synthesis
- / Anti-tumor
- / Crystal structure
English
Design,synthesis and anti-tumoractivity of novel amidine derivatives of doxifluridine
Abstract:
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.
-
Key words:
- Doxifluridine
- / Amidine
- / Synthesis
- / Anti-tumor
- / Crystal structure
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