新型萘醌衍生物的合成及生物评价。
Synthesis and Biological Evaluation of New Naphthoquinones Derivatives.
机构信息
Universite Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont-Ferrand, France.
Universite Hassan II Casablanca, FST, Laboratoire de Chimie Physique et Chimie Bio organique BP 146,28800 Mohammedia, Morocco.
出版信息
Curr Org Synth. 2020;17(3):224-229. doi: 10.2174/1570179417666200212111956.
UNLABELLED
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.
未标记
通过萘酚路线，制备了一系列新的取代 1,4-萘醌，总收率较高。这些化合物的细胞毒性在 MCF-7 乳腺癌细胞上进行了体外测试。最活跃的化合物 14 的 IC50 为 15μM。
目的
研究新型萘醌衍生物对 MCF-7 细胞的细胞毒性。
方法
合成新型萘醌衍生物，并在 MCF-7 细胞（resazurin 基于细胞的测定法）上评估其体外细胞毒性。
结果
从乙基 4-羟基-6,7-二甲氧基-2-萘酸酯出发，制备了四种萘醌，并对 MCF-7 细胞表现出显著的细胞毒性。
结论
结构-活性关系的初步研究表明了结构参数的影响，特别是萘醌侧链的性质。
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