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Research ArticleArticle

Novel Stable Camptothecin Derivatives Replacing the E-Ring Lactone by a Ketone Function Are Potent Inhibitors of Topoisomerase I and Promising Antitumor Drugs

Amélie Lansiaux, Stéphane Léonce, Laurence Kraus-Berthier, Christine Bal-Mahieu, Romain Mazinghien, Sébastien Didier, Marie-Hélène David-Cordonnier, Patrick Hautefaye, Gilbert Lavielle, Christian Bailly, John A. Hickman and Alain Pierré
Molecular Pharmacology August 2007, 72 (2) 311-319; DOI: https://doi.org/10.1124/mol.107.034637
Amélie Lansiaux
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Stéphane Léonce
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Laurence Kraus-Berthier
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Christine Bal-Mahieu
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Romain Mazinghien
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Sébastien Didier
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Marie-Hélène David-Cordonnier
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Patrick Hautefaye
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Gilbert Lavielle
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Christian Bailly
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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John A. Hickman
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Alain Pierré
Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
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Article Information

vol. 72 no. 2 311-319
DOI 
https://doi.org/10.1124/mol.107.034637
PubMed 
17494837

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0026-895X
Online ISSN 
1521-0111
History 
  • Received February 5, 2007
  • Accepted May 9, 2007
  • Published online July 24, 2007.

Article Versions

  • Earlier version (May 9, 2007 - 10:41).
  • You are viewing the most recent version of this article.
Copyright & Usage 
The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Amélie Lansiaux,
  2. Stéphane Léonce,
  3. Laurence Kraus-Berthier,
  4. Christine Bal-Mahieu,
  5. Romain Mazinghien,
  6. Sébastien Didier,
  7. Marie-Hélène David-Cordonnier,
  8. Patrick Hautefaye,
  9. Gilbert Lavielle,
  10. Christian Bailly1,
  11. John A. Hickman, and
  12. Alain Pierré
  1. Institut National de la Santé et de la Recherche Médicale U837, Université de Lille 2, Facultéde Médecine, Institut de Médecine Prédictive et Recherche Thérapeutique, Centre Oscar Lambret and Institut de Recherches sur le Cancer de Lille, Lille, France (A.L., C.B.-M., R.M., S.D., M.-H.D.-C., C.B.); and Division of Cancer Drug Discovery, Institut de Recherches Servier, Croissy sur Seine, France (S.L., L.K.-B., P.H., G.L., J.A.H., A.P.)
  1. Address correspondence to:
    Dr. Amélie Lansiaux, INSERM U-837 and Centre Oscar Lambret, ICRL, 59045 Lille, France. E-mail: amelie.lansiaux{at}lille.inserm.fr
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Molecular Pharmacology: 72 (2)
Molecular Pharmacology
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Research ArticleArticle

Novel Stable Camptothecin Derivatives Replacing the E-Ring Lactone by a Ketone Function Are Potent Inhibitors of Topoisomerase I and Promising Antitumor Drugs

Amélie Lansiaux, Stéphane Léonce, Laurence Kraus-Berthier, Christine Bal-Mahieu, Romain Mazinghien, Sébastien Didier, Marie-Hélène David-Cordonnier, Patrick Hautefaye, Gilbert Lavielle, Christian Bailly, John A. Hickman and Alain Pierré
Molecular Pharmacology August 1, 2007, 72 (2) 311-319; DOI: https://doi.org/10.1124/mol.107.034637

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Research ArticleArticle

Novel Stable Camptothecin Derivatives Replacing the E-Ring Lactone by a Ketone Function Are Potent Inhibitors of Topoisomerase I and Promising Antitumor Drugs

Amélie Lansiaux, Stéphane Léonce, Laurence Kraus-Berthier, Christine Bal-Mahieu, Romain Mazinghien, Sébastien Didier, Marie-Hélène David-Cordonnier, Patrick Hautefaye, Gilbert Lavielle, Christian Bailly, John A. Hickman and Alain Pierré
Molecular Pharmacology August 1, 2007, 72 (2) 311-319; DOI: https://doi.org/10.1124/mol.107.034637
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