A series of thirteen 5H-dibenzo [b,e][1,4]diazepin-11(10H)-one structural derivatives has been synthesized and evaluated for anti-proliferative activity against five human cancer cell lines. Compound 9a exhibited potent tumour growth inhibition in all cell lines with IC₅₀ values in the range of 0.71–7.29 μM. Experiments on lung (A549) and breast (MDAMB-231) cancer cell lines to investigate the mechanisms of growth inhibition and apoptosis inducing effects of 9a showed that it arrested both cancer cell lines in the G2/M phase of cell cycle in a dose dependent manner. Hoechst staining analysis revealed that 9a inhibited tumour cell proliferation through apoptosis induction. Additionally, the mitochondrial membrane potential (ΔΨm) was affected and the levels of reactive oxygen species (ROS) were raised. The simple synthetic preparation and their biological properties make these dibenzodiazepinone-triazole scaffolds promising new entities for the development of cancer therapeutics.

已经合成了一系列13个5 H-二苯并[ b，e ] [1,4]二氮杂11-11（10 H）-一个结构衍生物，并评估了其对五种人类癌细胞系的抗增殖活性。化合物9a在所有细胞系中均显示出有效的肿瘤生长抑制作用，IC ₅₀值在0.71-7.29μM的范围内。在肺癌（A549）和乳腺癌（MDAMB-231）细胞系上进行的实验研究了9a的生长抑制和凋亡诱导作用的机制，结果表明它以剂量依赖的方式在细胞周期的G2 / M期阻滞了这两种癌细胞系方式。Hoechst染色分析显示9a通过凋亡诱导抑制肿瘤细胞的增殖。此外，线粒体膜电位（ΔΨm）受到影响，活性氧（ROS）的水平升高。简单的合成方法及其生物学特性使这些二苯并二氮杂酮-三唑支架有望成为癌症治疗学发展的新实体。