18871-66-4Relevant articles and documents
Design, synthesis and anti-tumoractivity of novel amidine derivatives of doxifluridine
Feng, Ji Lu,Sun, Hai Ling,Geng, Dong Ping,Li, Ke
, p. 163 - 166 (2010)
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 52 μM 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.
Novel and efficient one-pot synthesis of N'-alkyl-N,N-dimethylacetamidines
Li, Zhe-Qi,Wang, Hui-Long
, p. 119 - 120 (2011)
An efficient method for the synthesis of N'-alkyl-N,N-dimethylacetamidine derivatives under mild conditions and in excellent yields involved reacting primary alkylamines with N,N-dimethylacetamide in the presence of LiCl as a catalyst and methanol as the acetalising reagent.
HETEROCYCLIC INDOLE DERIVATIVES AND MONO- OR DIAZAINDOLE DERIVATIVES
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, (2008/06/13)
Indole derivatives and mono- or diazaindole derivatives represented by general formula (1), pharmaceutically acceptable acid-addition salts or base-addition salts thereof or hydrates of the same which have a COX-2 inhibitory activity and are useful as drugs such as anti-inflammatory agents, wherein Het represents an optionally substituted heterocycle; A1 and A2 independently represent each -CH=, etc.; A3 represents -CH2-, etc.; R1 represents 4-fluorophenyl, etc.; R2 represents alkyl; and n is 0, 1 or 2, provided that when A1 and A2 are both -CH=, then A3 is -CH2- or -SO2-.
