ABSTRACT

In recent years, ruthenium (II) complexes have attracted attention due to high DNA topoisomerase I inhibitory activities and good anticancer activities. Herein, an asymmetric ligand 2-(5-(1, 10-phenanthroline))-1 H-4,5-diphenyl-imidazole (pdpi) and its ruthenium complexes were synthesized. DNA-binding mode of two complexes was determined as intercalation by using UV–vis spectra, emission spectra, viscosity, and molecular docking experiments. DNA photocleavage experimental results show that two ruthenium complexes effectively cleave plasmid DNA by producing singlet oxygen. Furthermore, they both displayed good topo I inhibition activities. The cytotoxic activities results show that complex 2 displays better antitumor activities against Eca-109 cells and A549 cells (IC₅₀ = 25.97 ± 3.33 μM and 28.83 ± 2.49 μM, respectively) compared to complex 1.

摘要

近年来，由于高的DNA拓扑异构酶I抑制活性和良好的抗癌活性，钌（II）复合物引起了人们的注意。在此，合成了不对称配体2-（5-（1，10-菲咯啉））-1H-4，5-二苯基咪唑（pdpi）及其钌络合物。通过使用紫外可见光谱，发射光谱，粘度和分子对接实验，将两种复合物的DNA结合模式确定为插入。DNA光裂解实验结果表明，两种钌配合物可通过产生单线态氧来有效裂解质粒DNA。此外，它们都显示出良好的topo I抑制活性。细胞毒性活性结果表明，复合物2对Eca-109细胞和A549细胞具有更好的抗肿瘤活性（IC ₅₀ 与络合物1相比，分别为25.97±3.33μM和28.83±2.49μM 。