[The solid-phase synthesis of methotrexate-alpha-peptides].

Methotrexate(MTX) and the methotrexate α peptides(MTX α phenylalanine and MTX α arginine ie. MTX α Phe and MTX α Arg) were prepared with the technique of solid phase peptide synthesis. Its purity was verified as a single peak by HPLC and its molecular weight was measured by mass spectrometry. MTX α Phe could be hydrolyzed to MTX by carboxypeptidase A. The cytotoxic effect of released MTX was found to be 100 times stronger than that of the peptide in vitro . It is suggested that MTX α Phe is a satisfactory prodrug in the treatment of cancer.