2. Academic Validation
  3. Synthesis and antitumor activity of 5-deaza-5,6,7,8-tetrahydrofolic acid and its N10-substituted analogues

Synthesis and antitumor activity of 5-deaza-5,6,7,8-tetrahydrofolic acid and its N10-substituted analogues

  • J Med Chem. 1989 Jul;32(7):1517-22. doi: 10.1021/jm00127a019.
E C Taylor 1,  J M Hamby,  C Shih,  G B Grindey,  S M Rinzel,  G P Beardsley,  R G Moran
Affiliations

Affiliation

  • 1 Department of Chemistry, Princeton University, New Jersey 08544.
PMID: 2738886 DOI: 10.1021/jm00127a019
Abstract

Syntheses of 5-deaza-5,6,7,8-tetrahydrofolic acid (7a) and its 10-formyl (7b), 10-acetyl (7c), and 10-methyl (7d) derivatives are described. These compounds, prepared as analogues of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF), the lead compound of a new class of folate antimetabolites, exhibit potent growth inhibition against leukemic cells in culture as well as substantial antitumor activity against transplantable murine solid tumors in vivo.

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