The ornithine (6a) and lysine (6b) analogues of methotrexate (1) have been synthesized via condensation of 4-amino-4-deoxy-N10-methylpteroic acid (2) with Nδ-carbobenzoxy-l-ornithine tert-butyl ester (3a) and Nϵ-carbobenzoxy-l-lysine tert-butyl ester (3b), respectively. Removal of the protecting groups gave 6a and 6b. Compounds 6a and 6b and their precursor Cbz acids (5a and 5b) show significant inhibition of dihydrofolate reductase.
|Original language||English (US)|
|Number of pages||3|
|Journal||Journal of Medicinal Chemistry|
|State||Published - Jan 1 1982|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery