Thilak Babu Lavanya, Paira Priyankar
Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology, Vellore 632014, Tamil Nadu, India.
ACS Omega. 2023 Aug 30;8(36):32382-32395. doi: 10.1021/acsomega.3c01639. eCollection 2023 Sep 12.
To enhance the cytoselective behavior of the complexes, we intended to develop a CuAAC "click"-derived synthetic protocol for the preparation of 2-(2-(4-(4-(pyridin-2-yl)-1-1,2,3-triazol-1-yl)butoxy)phenyl)benzo[]thiazole-based Ru(II)/Ir(III)/Re(I) complexes, and their cytotoxicity against three different cancer cell lines (MCF-7, HeLa, and U87MG) in consort with one normal cell line (HEK-293) was evaluated. In our detailed investigations, the significant cytotoxic nature of the Ru(II) complex compared to Ir(III) and Re(I) complexes ( and , respectively) was observed. Complex was capable of MCF-7 cell apoptosis via the inhibition of both S- and G2/M-phase cell cycle arrest in association with a substantial quantity of ROS production and DNA intercalation.
为了增强配合物的细胞选择性行为,我们打算开发一种基于铜催化的叠氮-炔环加成(CuAAC)“点击”反应的合成方法,用于制备基于2-(2-(4-(4-(吡啶-2-基)-1,2,3-三唑-1-基)丁氧基)phenyl)苯并噻唑的Ru(II)/Ir(III)/Re(I)配合物,并评估了它们对三种不同癌细胞系(MCF-7、HeLa和U87MG)以及一种正常细胞系(HEK-293)的细胞毒性。在我们的详细研究中,观察到Ru(II)配合物与Ir(III)和Re(I)配合物(分别为和)相比具有显著的细胞毒性。配合物能够通过抑制S期和G2/M期细胞周期停滞,同时产生大量活性氧(ROS)和DNA插入,诱导MCF-7细胞凋亡。