THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDES

PT Shi, XK Hao, Y Chen, YH Zhang , QY Tao, . THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDESJ. Acta Pharmaceutica Sinica, 1997, 32(2): 106-109.

Citation:

PT Shi, XK Hao, Y Chen, YH Zhang , QY Tao, . THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDESJ. Acta Pharmaceutica Sinica, 1997, 32(2): 106-109.

Citation:

PT Shi, XK Hao, Y Chen, YH Zhang , QY Tao, . THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDESJ. Acta Pharmaceutica Sinica, 1997, 32(2): 106-109.

Abstract

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.

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