Synthesis and Biological Evaluation of New Naphthoquinones Derivatives

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  • El-Mahdi Ourhzif
    Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, France
  • Caroline Decombat
    Universite Clermont Auvergne, INRA, Unite de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, France
  • Isabelle Abrunhosa-Thomas
    Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, France
  • Laetitia Delort
    Universite Clermont Auvergne, INRA, Unite de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, France
  • Mostafa Khouili
    Universite Sultan Moulay Slimane, FST, Laboratoire de Chimie Organique et Analytique, BP 523 Beni-Mellal, Morocco
  • Mohamed Akssira
    Universite Hassan II Casablanca, FST, Laboratoire de Chimie Physique et Chimie Bio organique BP 146,28800 Mohammedia, Morocco
  • Florence Caldefie-Chezet
    Universite Clermont Auvergne, INRA, Unite de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, France
  • Pierre Chalard
    Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, France
  • Yves Troin
    Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, France

Description

<jats:sec> <jats:title>:</jats:title> <jats:p>New substituted 1,4-naphthoquinones have been prepared in good overall yields through the naphthol route. The cytotoxicity of these compounds was tested in vitro on MCF-7 breast tumor cells. The most active compound 14 displayed an IC50 of 15μM.</jats:p> </jats:sec> <jats:sec> <jats:title>Objective:</jats:title> <jats:p>To investigate the cytotoxicity of new naphthoquinones derivatives on MCF-7 cells.</jats:p> </jats:sec> <jats:sec> <jats:title>Methods:</jats:title> <jats:p>Synthesis of new naphtoquinones derivatives and in vitro evaluation of their cytotoxicity on MCF-7 cells (rezasurin cell-based assay).</jats:p> </jats:sec> <jats:sec> <jats:title>Results:</jats:title> <jats:p>Starting from Ethyl 4-hydroxy-6,7-dimethoxy-2-naphthoate, four naphthoquinones were prepared and exhibited substantial cytotoxicity against MCF-7 cells.</jats:p> </jats:sec> <jats:sec> <jats:title>Conclusion:</jats:title> <jats:p>Preliminary studies of the structure-activity relationship have shown the influence of the structural parameters and, in particular, the nature of the naphthoquinone side chain.</jats:p> </jats:sec>

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