Corpus ID: 697633

Structural design, biochemical properties, and evidence for improved therapeutic activity of 5-alkyl derivatives of 5-deazaaminopterin and 5-deazamethotrexate compared to methotrexate in murine tumor models.

@article{Sirotnak1988StructuralDB,
  title={Structural design, biochemical properties, and evidence for improved therapeutic activity of 5-alkyl derivatives of 5-deazaaminopterin and 5-deazamethotrexate compared to methotrexate in murine tumor models.},
  author={F. Sirotnak and F. Schmid and G. Otter and J. Piper and J. Montgomery},
  journal={Cancer research},
  year={1988},
  volume={48 20},
  pages={
          5686-91
        }
}
  • F. Sirotnak, F. Schmid, +2 authors J. Montgomery
  • Published 1988
  • Chemistry, Medicine
  • Cancer research
  • Studies are described examining a new class of 4-aminofolate analogues modified by an N to C conversion and alkyl substitution at the N-5 position of aminopterin and methotrexate. All of these analogues were equivalent to aminopterin and methotrexate as inhibitors of tumor cell dihydrofolate reductase (Ki = 3.49-5.16 pM). N to C conversion at the N-5 position of aminopterin reduced its influx (inferred from the change in Ki) 3-fold, but the same modification increased influx of methotrexate 2-3… CONTINUE READING
    6 Citations

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