This study reports a facile synthesis and the cytotoxic evaluation of –H benzimidazoles. This synthetic method made use of the condensation reaction between -phenylenediamine and benzylamine and was highlighted by its solvent-free reaction conditions and short reaction time with the use of NaSO as an inexpensive and environmentally friendly oxidizing agent. The cytotoxicity assays revealed that the benzimidazole derivatives , , and displayed strong activity against the HeLa cancer cell line with the IC of 1.54 μM, 0.86 μM, and 1.03 μM, respectively, which were 5.6-fold, 10-fold, and 8-fold stronger than the positive control 5-fluorouracil (5-FU, IC = 8.61 μM). Furthermore, both compounds and exhibited similar cytotoxicities against MCF-7, which were equivalent to that of 5-FU and about 2.5-fold stronger than 5-FU towards the A549 cell line.

中文翻译：

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苯并咪唑衍生物的简易合成和细胞毒性评价的无溶剂策略

本研究报告了 –H 苯并咪唑的简便合成和细胞毒性评估。该合成方法利用对苯二胺和苄胺之间的缩合反应，并使用Na2SO4作为廉价且环保的氧化剂，具有无溶剂反应条件和短反应时间的特点。细胞毒性实验表明，苯并咪唑衍生物 、 、 和 对 HeLa 癌细胞系表现出较强的活性，IC 值分别为 1.54 μM、0.86 μM 和 1.03 μM，分别是 5.6 倍、10 倍和 8 倍强于阳性对照 5-氟尿嘧啶 (5-FU, IC = 8.61 μM)。此外，这两种化合物对MCF-7表现出相似的细胞毒性，与5-FU的细胞毒性相当，并且对A549细胞系的细胞毒性比5-FU强约2.5倍。