Synthesis and biological evaluation of new naphthoquinones derivatives
2020
Ourhzif, E. M. | Decombat, C. | ABRUNHOSA-THOMAS, I. | Delort, Laetitia | Khouili, M. | Akssira, M. | Caldefie-Chezet, Florence | Chalard, P. | Troin, Y.
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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