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Synthesis and Biological Evaluation of New Naphthoquinones Derivatives.
Current Organic Synthesis ( IF 1.8 ) Pub Date : 2020-05-01 , DOI: 10.2174/1570179417666200212111956
El-Mahdi Ourhzif 1, 2 , Caroline Decombat 3 , Isabelle Abrunhosa-Thomas 1 , Laetitia Delort 3 , Mostafa Khouili 4 , Mohamed Akssira 2 , Florence Caldefie-Chezet 3 , Pierre Chalard 1 , Yves Troin 1
Affiliation  

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.



中文翻译:

新萘醌衍生物的合成和生物学评价。

通过萘酚途径已经以良好的总收率制备了新的取代的1,4-萘醌。在体外对MCF-7乳腺肿瘤细胞测试了这些化合物的细胞毒性。活性最高的化合物14的IC50为15μM。

目的:研究新萘醌衍生物对MCF-7细胞的细胞毒性。

方法:合成新的萘醌衍生物,并体外评估其对MCF-7细胞的细胞毒性(基于可瑞沙林的细胞测定)。

结果:从4-羟基-6,7-二甲氧基-2-萘甲酸乙酯开始,制备了四种萘醌,并显示出对MCF-7细胞的实质性细胞毒性。

结论:对结构-活性关系的初步研究显示了结构参数的影响,尤其是萘醌侧链的性质。

更新日期:2020-05-01
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