Department of Chemistry, School of advanced sciences, Vellore Institute of Technology Vellore, 632014, Tamilnadu, India.
Department Stem Cells and Regenerative Medicine Centre, Institution Yenepoya Research Centre, Yenepoya University, University Road, Derlakatte, Mangalore 575018, Karnataka, India.
Dalton Trans. 2021 Jan 27;50(3):979-997. doi: 10.1039/d0dt03107k.
For diagnosing and annihilating cancer in the human body, herein, we have adopted a one pot convenient synthetic protocol to synthesize a library of half sandwich Ru(ii)-p-cymene-N^N complexes under continuous sonication and isolated their regioisomers by preparative thin layer chromatography followed by justification of stability using DFT. The present work has resulted in a library of ruthenium arene complexes and their isolated regioisomers following environmentally benign green processes and their screening of anticancer activity in terms of cytotoxicity and selectivity against cancer cell lines where [(η6-p-cymene)RuCl{2-(5,6-dichloro-1H-benzo[d]imidazole-2-yl)quinolone}] (11j) has been elicited to be significantly more potent as well as selective in Caco-2 and HeLa cell lines than the normal HEK-293 cell line compared to cisplatin and it has even shown marked cytotoxicity against the more aggressive HT-29 colorectal cancer cell line being capable of producing oxidative stress or arresting the cell cycle. Moreover, these types of Ru(ii)-arene complexes exhibited excellent binding efficacy with DNA and the compounds [(η6-p-cymene)RuCl{5-chloro-2-(6-(4-chlorophenyl)pyridin-2-yl)benzo[d]thiazole}]PF6 (8l4), [(η6-p-cymene)Ru-2-(6-(benzofuran-2-yl)pyridin-2-yl)-5-chlorobenzo[d]thiazole (8l9) and [(η6-p-cymene)RuCl{2-(6-nitro-1H-benzo[d]imidazol-2-yl)quinolone}]Cl (11f') and might be applied for cancer theranostic treatment due to their good fluorescence properties and remarkable potency.
为了在人体中诊断和消灭癌症，在这里，我们采用了一种一锅法的简便合成方案，在连续超声作用下合成了一系列半三明治 Ru(ii)-p-枯烯-N^N 配合物库，并通过制备性薄层层析分离其区域异构体，然后使用 DFT 对其稳定性进行了验证。本工作采用环境友好的绿色工艺得到了一系列钌芳基配合物及其分离的区域异构体，并对其进行了抗癌活性筛选，以细胞毒性和对癌细胞系的选择性为指标，其中[(η6-p-枯烯)RuCl{2-(5,6-二氯-1H-苯并[d]咪唑-2-基)喹啉}]（11j）在 Caco-2 和 HeLa 细胞系中比正常 HEK-293 细胞系更有效且更具选择性，与顺铂相比，它甚至对更具侵袭性的 HT-29 结直肠癌细胞系表现出显著的细胞毒性，能够产生氧化应激或阻止细胞周期。此外，这些类型的 Ru(ii)-芳基配合物与 DNA 具有优异的结合效力，化合物[(η6-p-枯烯)RuCl{5-氯-2-(6-(4-氯苯基)吡啶-2-基)苯并[d]噻唑}]PF6（8l4）、[(η6-p-枯烯)Ru-2-(6-(苯并呋喃-2-基)吡啶-2-基)-5-氯苯并[d]噻唑（8l9）和[(η6-p-枯烯)RuCl{2-(6-硝基-1H-苯并[d]咪唑-2-基)喹啉}]Cl（11f'）可能由于其良好的荧光性质和显著的效力而应用于癌症治疗。
