Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin

  • J Med Chem. 1985 Jul;28(7):914-21. doi: 10.1021/jm00145a012.
E C Taylor ,  P J Harrington ,  S R Fletcher ,  G P Beardsley ,  R G Moran
PMID: 4009615 DOI: 10.1021/jm00145a012
Abstract

Total syntheses from pyridine precursors of 5,10-dideazaaminopterin (1) and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin (2) are described. These compounds exhibit significant in vivo activity against L1210 leukemia that is comparable to that observed with methotrexate.

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