Literature DB >> 2738886

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

E C Taylor1, J M Hamby, C Shih, G B Grindey, S M Rinzel, G P Beardsley, R G Moran.   

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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Year:  1989        PMID: 2738886     DOI: 10.1021/jm00127a019

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Therapeutics by cytotoxic metabolite accumulation: pemetrexed causes ZMP accumulation, AMPK activation, and mammalian target of rapamycin inhibition.

Authors:  Alexandra C Racanelli; Scott B Rothbart; Cortney L Heyer; Richard G Moran
Journal:  Cancer Res       Date:  2009-06-23       Impact factor: 12.701

2.  Mechanism of cytotoxicity of 5,10-dideazatetrahydrofolic acid in human ovarian carcinoma cells in vitro and modulation of the drug activity by folic or folinic acid.

Authors:  E Erba; S Sen; C Sessa; F L Vikhanskaya; M D'Incalci
Journal:  Br J Cancer       Date:  1994-02       Impact factor: 7.640

3.  Role of membrane folate-binding protein in the cytotoxicity of 5,10-dideazatetrahydrofolic acid in human ovarian carcinoma cell lines in vitro.

Authors:  S Sen; E Erba; M D'Incalci; F Bottero; S Canevari; A Tomassetti
Journal:  Br J Cancer       Date:  1996-02       Impact factor: 7.640

  3 in total

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