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Antitumour Activity and Pharmacology of CCRG 81010 (NSC 353451, M&B 39565, 8-carbamoyl-3-(1-chloroethyl)imidazo [5,1-d]-1,1,3,5-tetrazin-4(3H)-one)

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Cancer Chemotherapy and Selective Drug Development

Part of the book series: Developments in Oncology ((DION,volume 23))

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Abstract

CCRG 81010 is one of the most potently active experimental antitumour agents which has been tested against murine tumours in vivo and it accomplishes the cure of animals bearing most of the ascitic or solid tumours (1–3). The rationale for its synthesis and screening arose from long term interests in the chemistry and pharmacology of molecules which contain triazene (N-N-N) linkages (4,5) and in the pharmacology of the nitrosoureas (6). Figure 1 shows the structure of CCRG 81010 together with that of the clinically useful antitumour triazene DTIC and a generalised formula for the chloroethylnitrosoureas. Structural similarities are apparent and indeed these similarities have been shown to extend to the broad spectrum of antitumour activity demonstrated by CCRG 81010 and to its mechanism of action, both of which will be outlined here.

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References

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Authors

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K. R. Harrap W. Davis A. H. Calvert

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© 1984 Martinus Nijhoff Publishing, Boston

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Hickman, J.A., Stevens, M.F.G. (1984). Antitumour Activity and Pharmacology of CCRG 81010 (NSC 353451, M&B 39565, 8-carbamoyl-3-(1-chloroethyl)imidazo [5,1-d]-1,1,3,5-tetrazin-4(3H)-one). In: Harrap, K.R., Davis, W., Calvert, A.H. (eds) Cancer Chemotherapy and Selective Drug Development. Developments in Oncology, vol 23. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-3837-6_47

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  • DOI: https://doi.org/10.1007/978-1-4613-3837-6_47

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-3839-0

  • Online ISBN: 978-1-4613-3837-6

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