Inhibition of Thymidylate Synthetase by the New Quinazoline Antifolate, CB 3717; Enzyme Purification and Kinetics

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


CB 3717, N-(4-(N-((2-amino-4-hydroxy-6-quinazolinyl)methyl)prop-2-ynylamino)benzoyl)-L-glutamic acid is a novel antifolate designed as an inhibitor of thymidylate synthetase (TS).1 The propargyl substituent at the N10 position is critical for good enzyme inhibition. We have demonstrated that CB 3717 has TS as its sole cytotoxic locus both in vitro and in vivo.1,2,3


L1210 Cell Affinity Resin Carbodiimide Hydrochloride Thymidylate Synthetase Biomedical Computer Program 
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Copyright information

© Springer Science+Business Media New York 1984

Authors and Affiliations

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

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