Irreversible enzyme inhibitors. 200. Active-site-directed inhibitors of deoxycytidine kinase.
Forty-three pyrimidine derivatives, mainly containing the 4-aminopyrimidine system, have been prepared and evaluated as inhibitors of deoxycytidine kinase. The most effective inhibitors were 2-alkylthio-4-aminopyrimidines and 1-alky-1-cytosines. The best inhibitors in both groups were those with large alkyl substituents, which indicate that hydrophobic bonding is occurring, possibly in the same area adjacent to the active site.
D000478:Alkylation; D001665:Binding Sites; D055598:Chemical Phenomena; D002621:Chemistry; D003596:Cytosine / Q000031:analogs & derivatives; D003841:Deoxycytidine; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D010770:Phosphotransferases / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000138:chemical synthesis*
D004791:Enzyme Inhibitors; D011743:Pyrimidines; D003841:Deoxycytidine; D003596:Cytosine; D010770:Phosphotransferases