Musumeci Domenica, Roviello Giovanni N, Rigione Giuseppina, Capasso Domenica, Di Gaetano Sonia, Riccardi Claudia, Roviello Valentina, Montesarchio Daniela
Department of Chemical Sciences, University of Naples Federico II, Via Cintia 21, 80126, Naples, Italy.
Institute of Biostructures and Bioimaging, CNR, Via Mezzocannone 16, 80134, Naples, Italy.
Chempluschem. 2017 Feb;82(2):251-260. doi: 10.1002/cplu.201600547. Epub 2016 Nov 29.
To further explore the properties and bioactivity of benzodifurans, three compounds in this class were synthesised and characterised using spectroscopic and spectrometric techniques, as well as SEM and thermogravimetric analysis. The synthesised compounds showed interesting antiproliferative activity on different human cancer cells (HeLa, Hep-G2, WM266), whereas no relevant cytotoxic effect was observed on healthy control cells. To study the possible mechanism of action of the benzodifurans, their ability to bind various model DNA systems, their aggregation properties, and their ability to bind biologically relevant metal ions was evaluated. The molecules were found to form monodisperse nanoaggregates stable at physiological temperature, which are likely related to the observed bioactivity.
为了进一步探索苯并二呋喃的性质和生物活性，合成了该类中的三种化合物，并使用光谱和光谱技术以及扫描电子显微镜（SEM）和热重分析对其进行了表征。合成的化合物对不同的人类癌细胞（HeLa、Hep-G2、WM266）显示出有趣的抗增殖活性，而在健康对照细胞上未观察到相关的细胞毒性作用。为了研究苯并二呋喃可能的作用机制，评估了它们与各种模型DNA系统结合的能力、聚集特性以及与生物相关金属离子结合的能力。发现这些分子形成了在生理温度下稳定的单分散纳米聚集体，这可能与观察到的生物活性有关。
