Syntheses and antifolate activity of 5-methyl-5-deaza analogues of aminopterin, methotrexate, folic acid, and N10-methylfolic acid.

@article{Piper1986SynthesesAA,
  title={Syntheses and antifolate activity of 5-methyl-5-deaza analogues of aminopterin, methotrexate, folic acid, and N10-methylfolic acid.},
  author={J. Piper and G. Mccaleb and J. Montgomery and R. Kisliuk and Y. Gaumont and F. Sirotnak},
  journal={Journal of medicinal chemistry},
  year={1986},
  volume={29 6},
  pages={
          1080-7
        }
}
  • J. Piper, G. Mccaleb, +3 authors F. Sirotnak
  • Published 1986
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • Evidence indicating that modifications at the 5- and 10-positions of classical folic acid antimetabolites lead to compounds with favorable differential membrane transport in tumor vs. normal proliferative tissue prompted an investigation of 5-alkyl-5-deaza analogues. 2-Amino-4-methyl-3,5-pyridinedicarbonitrile, prepared by hydrogenolysis of its known 6-chloro precursor, was treated with guanidine to give 2,4-diamino-5-methylpyrido[2,3-d]pyrimidine-6-carbonitrile which was converted via the… CONTINUE READING
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