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Synthesis and biological evaluation of new naphthoquinones derivatives

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 15microM. OBJECTIVE: To investigate the cytotoxicity of new naphthoquinones derivatives on MCF-7 cells. METHOD: 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.
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Submitted on : Wednesday, March 4, 2020 - 8:10:55 PM
Last modification on : Tuesday, March 17, 2020 - 2:38:52 AM




E. M. Ourhzif, C. Decombat, I. Abrunhosa-Thomas, Laetitia Delort, M. Khouili, et al.. Synthesis and biological evaluation of new naphthoquinones derivatives. Current Organic Synthesis, Bentham Science Publishers, 2020, ⟨10.2174/1570179417666200212111956⟩. ⟨hal-02498986⟩



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