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Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.

Three new approaches have been tested to modify existing pyridopyrimidine and alkynylpyrimidine classes of nonnucleoside adenosine kinase inhibitors 2 and 3. 4-Amino-substituted pteridines 8a-e were generally less active than corresponding 5- and 6-substituted pyridopyrimidines 2. Pyrazolopyrimidine 13c with IC(50)=7.5 nM was superior to its open chain alkynylpyrimidine analog 13g (IC(50)=22 nM) while pyrrolopyrimidines such as 17a were inactive.[1]

References

  1. Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors. Gomtsyan, A., Didomenico, S., Lee, C.H., Stewart, A.O., Bhagwat, S.S., Kowaluk, E.A., Jarvis, M.F. Bioorg. Med. Chem. Lett. (2004) [Pubmed]
 
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