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Current Organic Synthesis

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ISSN (Print): 1570-1794
ISSN (Online): 1875-6271

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Research Article

Synthesis and Biological Evaluation of New Naphthoquinones Derivatives

Author(s): El-Mahdi Ourhzif , Caroline Decombat , Isabelle Abrunhosa-Thomas , Laetitia Delort , Mostafa Khouili, Mohamed Akssira *, Florence Caldefie-Chezet , Pierre Chalard and Yves Troin*

Volume 17, Issue 3, 2020

Page: [224 - 229] Pages: 6

DOI: 10.2174/1570179417666200212111956

Price: $65

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.

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