1. Antitumor and biological investigation of doubly cyclometalated ruthenium(II) organometallics derived from benzimidazolyl derivatives.
- Author
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Elumalai P, Jeong YJ, Park DW, Kim DH, Kim H, Kang SC, and Chi KW
- Subjects
- Antineoplastic Agents chemical synthesis, Cell Line, Tumor, Cell Proliferation drug effects, Cytokines metabolism, Drug Screening Assays, Antitumor, Drug Stability, Humans, Ligands, Models, Molecular, Molecular Conformation, Organometallic Compounds chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Benzimidazoles chemistry, Organometallic Compounds chemistry, Organometallic Compounds pharmacology, Ruthenium chemistry
- Abstract
In this study, we report the synthesis, anticancer and biological properties of three doubly cyclometalated phenylbenzimidazole derived ruthenium(ii) organometallics () and their corresponding three organic ligands. The structures of were fully characterized by various analytical techniques, and the meso stereoisomer of the doubly cyclometalated ruthenacycle was unambiguously confirmed by single crystal X-ray diffraction. The anticancer effects of the newly synthesized compounds were tested against selected human cancer cell lines AGS (gastric carcinoma), SK-hep-1 (hepatocellular carcinoma), and HCT-15 (colorectal carcinoma). The growth inhibitory effects of ruthenacycles on cancer cells were found to be considerably more effective against the abovementioned cancer cells than the reference drug oxaliplatin. Compound exhibited a more specific effect on the AGS cells. Gene-fishing and ELISA array were performed to analyze the target genes and cytokine secretion by . As a result, a significant reduction was observed in RPS21 by . Moreover, increased the secretion of cytokines such as IFNγ in macrophages and reduced the release of cytokines such as rantes and IGF-1. These results show that could be a very good anticancer drug through the regulation of the RPS21 gene and cytokines.
- Published
- 2016
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