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Abstract

In one embodiment, the present invention relates to a new class of ammonium salts of Nδ-acyl derivatives of Nα-(4-amino-4-deoxypteroyl)-L-ornithine compounds having a structure according to formula II-IV. Formula II has the structure of: ##STR1## wherein: R2 represents up to four groups independently selected at each occurrence of R2 from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C1-6 alkoxy, chloro, fluoro, hydroxy, and —COOH; R3, R4, and R5 are each independently selected from hydrogen and C1-6 alkyl; or NR3R4 taken combination can form a 5 to 7 member heterocycle having at least one nitrogen ring atom; and x is a real number greater than 0 and less than about 4. The ammonium salts provided by the invention exhibit high inhibitory activity against the growth o methotrexate-resistant cells, and also exhibit superior chemical stability than corresponding acidic Nδ-acyl derivatives of Nδ-acyl derivatives of Nα(4-amino-4-deoxypteroyl)-L-ornithine compounds.

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First Claim