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Synthesis and Biological Evaluation of New Naphthoquinones Derivatives

[ Vol. 17 , Issue. 3 ]

Author(s):

El-Mahdi Ourhzif , Caroline Decombat , Isabelle Abrunhosa-Thomas , Laetitia Delort , Mostafa Khouili, Mohamed Akssira *, Florence Caldefie-Chezet , Pierre Chalard and Yves Troin*   Pages 224 - 229 ( 6 )

Abstract:


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.

Objective: To investigate the cytotoxicity of new naphthoquinones derivatives on MCF-7 cells.

Methods: Synthesis of new naphtoquinones derivatives and in vitro evaluation of their cytotoxicity on MCF-7 cells (rezasurin cell-based assay).

Results: Starting from Ethyl 4-hydroxy-6,7-dimethoxy-2-naphthoate, four naphthoquinones were prepared and exhibited substantial cytotoxicity against MCF-7 cells.

Conclusion: 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.

Keywords:

Quinones, medicinal chemistry, cytotoxicity, antitumor agents, MCF-7 cells, naphthoquinones.

Affiliation:

Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, Universite Clermont Auvergne, INRA, Unite de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, Universite Clermont Auvergne, INRA, Unite de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, Universite Sultan Moulay Slimane, FST, Laboratoire de Chimie Organique et Analytique, BP 523 Beni-Mellal, Universite Hassan II Casablanca, FST, Laboratoire de Chimie Physique et Chimie Bio organique BP 146,28800 Mohammedia, Universite Clermont Auvergne, INRA, Unite de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand

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