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Notes on the Metabolism, Pharmacokinetics and Mode of Action of N-Methyl and N-Ethyl-Triazenes in Relation to Their Pharmacological Activity

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Triazenes

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Abstract

Dacarbazine (DTIC) is an antitumor agent which has a well documented activity against some human tumors 1, 2. Its preclinical and clinical activity is not striking, but is justified by its relatively low toxicity. As for most anticancer agents the molecular mode of action of dimethyltriazenes is still debatable but most authors recognize the importance of N-demethylation for the activation of these drugs 3, 4. The monoalkylderivative is probably the alkylating species responsible for the antitumor activity. Structure activity studies have essentially failed to find any new dimethyltriazene clearly superior to those already available. However, several studies have shown that diethyltriazenes are inactive. The reasons for the discrepant activity of dimethyltriazenes and diethyltriazenes is still unknown.

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Authors and Affiliations

  1. Istituto di Ricerche Farmacologiche “Mario Negri”, Via Eritrea 62, 20157, Milan, Italy

    Maurizio D’Incalci, Tina Colombo, Pierluigi Farina Cecilia Mannironi, Pietro Taverna & Carlo V. Catapano

Authors
  1. Maurizio D’Incalci
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  2. Tina Colombo
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  3. Pierluigi Farina Cecilia Mannironi
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  4. Pietro Taverna
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  5. Carlo V. Catapano
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Editor information

Editors and Affiliations

  1. Istituto di Farmacologia, Università di Trieste, 34127, Trieste, Italy

    Tullio Giraldi

  2. Toxicology Unit, Medical Research Council, Woodmansterne Road, SM5 4EF, Carshalton, Surrey, UK

    Thomas A. Connors

  3. Divisione di Oncologia Medica, Ospedale S. Maria della Misericordia, 33100, Udine, Italy

    Giuseppe Cartei

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© 1990 Springer Science+Business Media New York

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D’Incalci, M., Colombo, T., Mannironi, P.F.C., Taverna, P., Catapano, C.V. (1990). Notes on the Metabolism, Pharmacokinetics and Mode of Action of N-Methyl and N-Ethyl-Triazenes in Relation to Their Pharmacological Activity. In: Giraldi, T., Connors, T.A., Cartei, G. (eds) Triazenes. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3832-5_8

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  • DOI: https://doi.org/10.1007/978-1-4615-3832-5_8

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-6710-9

  • Online ISBN: 978-1-4615-3832-5

  • eBook Packages: Springer Book Archive

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