Methotrexate Analogues. 30. Dihydrofolate Reductase Inhibition and in Vitro Tumor Cell Growth Inhibition by Nε-(Haloacetyl)-L-lysine and Nδ-(Haloacetyl)-L-ornithine Analogues and an Acivicin Analogue of Methotrexate

Article abstract of DOI:10.1021/jm00391a031

Analogues of methotrexate (MTX) with strong alkylating activity were prepared by replacing the L-glutamate side chain with N^ω-haloacetyl derivatives of L-lysine and L-ornithine.Haloacetylation was accomplished in 30-40percent yield by reaction