Document Report Card

ID: ALA1124522

Journal: J Med Chem

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

Authors: Taylor EC, Hamby JM, Shih C, Grindey GB, Rinzel SM, Beardsley GP, Moran RG.

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.

CiteXplore: 2738886

DOI: 10.1021/jm00127a019