一种绿色方法合成喹喔啉和双喹喔啉及其对 A431（人皮肤癌细胞系）的生物评估。
A green approach toward quinoxalines and bis-quinoxalines and their biological evaluation against A431, human skin cancer cell lines.
机构信息
Department of Chemistry, The University of Texas-Pan American, 1201 West University Drive, Edinburg, Texas 78539, USA.
出版信息
Future Med Chem. 2013 Aug;5(12):1377-90. doi: 10.4155/fmc.13.101.
BACKGROUND
The objective of this study was to develop a practical green procedure to synthesize quinoxalines and bis-quinoxalines and evaluate their inhibitory effects on the viability of A431 human epidermoid carcinoma cells.
METHOD
A series of quinoxaline and bis-quinoxaline derivatives have been designed and synthesized following a microwave-assisted and bismuth nitrate-catalyzed eco-friendly route. A detailed comparison has been made between microwave-induced protocol with the reactions occurred at room temperature. The structure of the compounds have been elucidated by various spectroscopic methods and finally confirmed by x-ray crystallographic analyses.
RESULTS
Two quinoxaline derivatives, compounds 6 and 12 have demonstrated inhibitory effects on the viability of A431 human epidermoid carcinoma cells when compared with HaCaT nontumorigenic human keratinocyte cells.
CONCLUSION
Notably, compound 6 inhibits Stat3 phosphorylation/activation in A431 skin cancer cells.
背景
本研究旨在开发一种实用的绿色方法来合成喹喔啉和双喹喔啉，并评估它们对 A431 人表皮癌细胞活力的抑制作用。
方法
采用微波辅助和硝酸铋催化的环保路线，设计并合成了一系列喹喔啉和双喹喔啉衍生物。详细比较了微波诱导法与室温下反应的差异。通过各种光谱方法阐明了化合物的结构，并最终通过 X 射线晶体学分析得到了证实。
结果
与非肿瘤性人类角质形成细胞 HaCaT 相比，两种喹喔啉衍生物（化合物 6 和 12）对 A431 人表皮癌细胞的活力具有抑制作用。
结论
值得注意的是，化合物 6 可抑制 A431 皮肤癌细胞中 Stat3 的磷酸化/激活。
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