New bis‐2(5H)‐furanone derivatives containing a benzidine core were synthesized via a one‐step transition‐metal‐free reaction of benzidine with 5‐substituted 3,4‐dihalo‐2(5H)‐furanones. Their antitumor activities against various tumor cells have been evaluated by MTT assay. Among them, compound 4e exhibits significant inhibitory activity against C6 glioma cells with an IC₅₀ value of 12.1 μm and low toxicity toward HaCaT human normal cells. Studies on the antitumor mechanism reveal that cell cycle arrest at S‐phase in C6 cells is induced by compound 4e. Furthermore, investigations with electronic, fluorescence emission and circular dichroism spectra show that compound 4e can significantly interact with C6‐DNA. These data indicate that DNA may be one of the potential targets for bis‐2(5H)‐furanone derivatives as anticancer drugs.

中文翻译：

---

Bis-2（5H）-呋喃酮衍生物作为新型抗癌药：设计，合成，生物学评估和机理研究

通过联苯胺与5个取代的3,4-二卤代-2（5 H）-呋喃酮的一步无过渡金属反应，合成了新的含有联苯胺核心的bis-2（5 H）-呋喃酮衍生物。已经通过MTT测定法评估了它们对各种肿瘤细胞的抗肿瘤活性。其中，化合物4e中显示出了一个IC针对C6胶质瘤细胞显著抑制活性₅₀ 12.1μ值米和低毒性的HaCaT朝向人体正常细胞。有关抗肿瘤机制的研究表明，化合物4e可诱导C6细胞S期的细胞周期停滞。此外，对电子，荧光发射和圆二色性光谱的研究表明，化合物4e可以与C6-DNA发生显着相互作用。这些数据表明，DNA可能是bis-2（5 H）-呋喃酮衍生物作为抗癌药物的潜在靶标之一。