142836-70-2Relevant academic research and scientific papers
Latent Inhibitors. Part 8. Synthesis and Evaluation of some Mechanism-based Inhibitors of Dihydrofolate Reductase
McGill, John,Rees, Lilias,Suckling, Colin J.,Wood, Hamish C. S.
, p. 1299 - 1304 (2007/10/02)
The synthesis of two new pteridine-7-spirocyclopropanes that are time-dependent irreversible inhibitors of dihydrofolate reductase is described.Several related compounds including a cyclopropyl substituted quinoxaline and 2-aminopteridine-4(3H),6(5H)-dione were also prepared but these compounds were not found to be time-dependent inhibitors.The inhibitors were assessed using several dihydrofolate reductases, Escherichia coli RT/39, two mutants of the E. coli enzyme, Lactobacillus casei, and chicken liver.Activity was found against all enzymes tested but most strongly against E. coli wild type enzyme.
