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Antineoplastic activity of lipid-soluble dialkyl esters of methotrexate

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Résumé

L'action biologique de 6 esters liposolubles di-n-alkyle de la méthotrexate (MTX) a été comparée à celle du composé non estérifié. En tant qu'inhibiteurs de la réductase dihydrofolate de cellules leucémiques L1210 de la souris, les esters ont été moins efficaces que la MTX. In vivo, les esters dialkyles ont eu une action égale à celle de la MTX, en prolongeant la survie des souris inoculées par l'injection de cellules leucémiques L1210. Puisque les esters sont rapidement hydrolysés in vivo on conclut que l'action antitumeur chez la souris est due à la libération de la MTX.

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Authors and Affiliations

  1. Laboratory of Chemical Pharmacology, National Cancer Institute, 20014, Bethesda, Maryland, USA

    D. G. Johns, D. Farquhar, B. A. Chabner, M. K. Wolpert & R. H. Adamson

  2. Department of Developmental Therapeutics, The University of Texas at Houston, M.D. Anderson Hospital and Tumor Institute, 77025, Houston, Texas, USA

    D. G. Johns, D. Farquhar, B. A. Chabner, M. K. Wolpert & R. H. Adamson

Authors
  1. D. G. Johns
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  2. D. Farquhar
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  3. B. A. Chabner
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  4. M. K. Wolpert
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  5. R. H. Adamson
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Additional information

We thank Dr.Dorris J. Hutchison, Sloan-Kettering Institute for Cancer Research, for supplying mice bearing the L1210/A (XL) tumor; and Mr.C. J. Derr, Mr.J. C. Drake and Mr.S. T. Yancey for skilled technical assistance.

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Johns, D.G., Farquhar, D., Chabner, B.A. et al. Antineoplastic activity of lipid-soluble dialkyl esters of methotrexate. Experientia 29, 1104–1105 (1973). https://doi.org/10.1007/BF01946745

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  • DOI: https://doi.org/10.1007/BF01946745

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