Inhibition of Mammalian Folylpolyglutamate Synthetase and Human Dihydrofolate Reductase by 5,8-Dideaza Analogues of Folic Acid and Aminopterin Bearing a Terminal L-Ornithine

Article abstract of DOI:10.1021/jm00127a026

Six new 5,8-dideaza analogues of folic acid and aminopterin containing a terminal L-ornithine residue were prepared by using multistep synthetic sequences.Each was evaluated as an inhibitor of hog liver folylpolyglutamate synthetase and human dihydrofolat