Lysine and ornithine analogs of methotrexate as inhibitors of dihydrofolate reductase

Publisher Website
Google Scholar
Abstract
The ornithine (6a) and lysine (6b) analogs of [the anticancer drug] methotrexate were synthesized via condensation of 4-amino-4-deoxy-N10-methylpteroic acid with N.delta.-carbobenzoxy-L-ornithine tert-butyl ester and N.epsilon.-carbobenzoxy-L-lysine tert-butyl ester, respectively. Removal of the protecting groups gave 6a and 6b. Compounds 6a and 6b and their precursor Cbz [carbobenzoxy] acids show significant inhibition of dihydrofolate reductase.