Studies on the Inhibition of Bovine Liver Dihydrofolate
Reductase by Pyrimidine Compounds
王惠珀
Cheng CY;Wang HP
Abstract
A series of 6-slky1-2,4-diaminopyrimidines (compounds 1- 5) and 6- methylamino-2,4-diaminopyimidines (copounds 6-12), prepared as nonclassical folate antimetabolites, were subjected to inhibition study on bovine liver dihydrofolate reductase. The 2,4-diaminopyrimidine compounds showed IC50's at 10-7-10-9M, with compound 5 as the most acitve showing comparable activity to that of methotrexate. The triaminopyrimidine analogues 6-12 were much less active, with IC50's ranged between 10-4-10-6 M.