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Article Dans Une Revue Current Organic Synthesis Année : 2020

Synthesis and biological evaluation of new naphthoquinones derivatives

Résumé

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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hal-02498986 , version 1 (04-03-2020)

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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, 2020, 17 (3), pp.224-229. ⟨10.2174/1570179417666200212111956⟩. ⟨hal-02498986⟩
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