Plasma Nucleoside and Base Levels Following Treatment with the New Thymidylate Synthetase Inhibitor CB 3717

  • G. A. Taylor
  • A. L. Jackman
  • A. H. Calvert
  • K. R. Harrap
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 165)

Abstract

CB 3717 (N-(4-(N-((2-amino-4-hydroxy-6-quinazolinyl)methyl)prop-2-ynylamino)benzoyl)-L-glutamic acid), a quinazoline antifolate, is a potent inhibitor of thymidylate synthetase (TS).1 Investigations have revealed that TS is its sole cytotoxic locus both in vivo and in vitro. 2–4 This drug possesses considerable advantages in comparison to other antimetabolites affecting thymidine triphosphate (TTP) production.3

Keywords

High Performance Liquid Chromatographic Lymphoma Folate Succinate Pyrimidine 

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References

  1. 1.
    A.L. Jackman, A.H. Calvert, L.I. Hart and K.R. Harrap, Inhibition of thymidylate synthetase by the new quinazoline antifolate CB 3717, See this volume.Google Scholar
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    T.R. Jones, A.H. Calvert, A.L, Jackman, S.J. Brown, M. Jones and K.R. Harrap, A potent antitumour quinazoline inhibitor of thymidylate synthetase, Europ. J. Cancer 17: 11 (1981).Google Scholar
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    A.L. Jackman, G.A. Taylor, D.R. Newell, A.H. Calvert and K.R. Harrap, Biochemical disturbances observed in vitro and in vivo following inhibition of thymidylate synthetase by CB 3717, Brit. J.Cancer (1982) in press.Google Scholar
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    J. Maybaum, M.B. Cohen and W. Sadee, In vivo rates of pyrimidine nucleotide metabolism in intact mouse T lymphoma (S-49) cells treated with 5-fluorouracil, J. Biol. Chem. 256: 2126 (1981).PubMedGoogle Scholar
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    R.C. Jackson, Biochemical effects of the quinazoline antifolate CB 3717 on human lymphoblastoid cells, Proc. Am. Ass. Cancer Res. 80: 713 (1982).Google Scholar

Copyright information

© Springer Science+Business Media New York 1984

Authors and Affiliations

  • G. A. Taylor
    • 1
  • A. L. Jackman
    • 1
  • A. H. Calvert
    • 1
  • K. R. Harrap
    • 1
  1. 1.Department of Biochemical PharmacologyInstitute of Cancer ResearchSutton, SurreyEngland

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