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6-Halogenochromones Bearing Tryptamine: One-Step Access to Potent and Highly Selective Inhibitors of Breast Cancer Resistance Protein

Authors

  • Glaucio Valdameri,

    1. Mechanisms and Modulation of Drug Resistance Team, Institute of Biology and Chemistry of Proteins, BMSSI UMR 5086 CNRS/University of Lyon 1, 7 Passage du Vercors, 69367 Lyon (France)
    2. Department of Biochemistry and Molecular Biology, Federal University of Paraná, Centro Politécnico, Jardim da Américas, 81531-980 Curitiba, PR (Brazil)
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    • These junior authors contributed equally to this work.

  • Dr. Estelle Genoux-Bastide,

    1. Department of Molecular Medicinal Chemistry, Université Joseph Fourier-Grenoble 1/CNRS UMR 5063, Bâtiment E André Rassat, Pôle Chimie, BP 53, 38041 Grenoble (France)
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    • These junior authors contributed equally to this work.

  • Charlotte Gauthier,

    1. Mechanisms and Modulation of Drug Resistance Team, Institute of Biology and Chemistry of Proteins, BMSSI UMR 5086 CNRS/University of Lyon 1, 7 Passage du Vercors, 69367 Lyon (France)
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  • Basile Peres,

    1. Department of Molecular Medicinal Chemistry, Université Joseph Fourier-Grenoble 1/CNRS UMR 5063, Bâtiment E André Rassat, Pôle Chimie, BP 53, 38041 Grenoble (France)
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  • Dr. Raphaël Terreux,

    1. Bioinformatics: Structure and Interactions Team, Institute of Biology and Chemistry of Proteins, BMSSI UMR 5086 CNRS/University of Lyon 1, 7 Passage du Vercors, 69367 Lyon (France)
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  • Prof. Sheila M. B. Winnischofer,

    1. Department of Biochemistry and Molecular Biology, Federal University of Paraná, Centro Politécnico, Jardim da Américas, 81531-980 Curitiba, PR (Brazil)
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  • Prof. Maria E. M. Rocha,

    1. Department of Biochemistry and Molecular Biology, Federal University of Paraná, Centro Politécnico, Jardim da Américas, 81531-980 Curitiba, PR (Brazil)
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  • Dr. Attilio Di Pietro,

    1. Mechanisms and Modulation of Drug Resistance Team, Institute of Biology and Chemistry of Proteins, BMSSI UMR 5086 CNRS/University of Lyon 1, 7 Passage du Vercors, 69367 Lyon (France)
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    • These senior authors contributed equally to this work.

  • Prof. Ahcène Boumendjel

    Corresponding author
    1. Department of Molecular Medicinal Chemistry, Université Joseph Fourier-Grenoble 1/CNRS UMR 5063, Bâtiment E André Rassat, Pôle Chimie, BP 53, 38041 Grenoble (France)
    • Department of Molecular Medicinal Chemistry, Université Joseph Fourier-Grenoble 1/CNRS UMR 5063, Bâtiment E André Rassat, Pôle Chimie, BP 53, 38041 Grenoble (France)
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    • These senior authors contributed equally to this work.


Abstract

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Easy as A B C! 6-Halochromone derivatives bearing a tryptamine moiety were evaluated as inhibitors of the breast cancer resistance protein (BCRP)/ABCG2. The 6-bromo analogue has been identified as a highly potent, selective and nontoxic inhibitor of BCRP. The facile synthesis from commercial starting materials makes this inhibitor an ideal candidate for preclinical investigations.

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