title: Antitumor and biological investigation of doubly cyclometalated ruthenium(II) organometallics derived from benzimidazolyl derivatives.
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.
authors.affiliation: Department of Chemistry, University of Ulsan, Ulsan 680-749, Republic of Korea. kwchi@ulsan.ac.kr.
authors.forename: Palani
authors.initials: P
authors.lastname: Elumalai
authors.affiliation: Department of Oriental Medicinal Material & Processing, College of Life Science, Kyung Hee University, Yongin 17104, Republic of Korea. sckang@khu.ac.kr.
authors.forename: Yong Joon
authors.initials: YJ
authors.lastname: Jeong
authors.affiliation: Department of Oriental Medicinal Material & Processing, College of Life Science, Kyung Hee University, Yongin 17104, Republic of Korea. sckang@khu.ac.kr.
authors.forename: Dae Won
authors.initials: DW
authors.lastname: Park
authors.affiliation: Department of Chemistry, University of Ulsan, Ulsan 680-749, Republic of Korea. kwchi@ulsan.ac.kr.
authors.forename: Dong Hwan
authors.initials: DH
authors.lastname: Kim
authors.affiliation: Energy Materials Lab, Korea Institute of Energy Research, Daejeon 305-343, Republic of Korea.
authors.forename: Hyunuk
authors.initials: H
authors.lastname: Kim
authors.affiliation: Department of Oriental Medicinal Material & Processing, College of Life Science, Kyung Hee University, Yongin 17104, Republic of Korea. sckang@khu.ac.kr.
authors.forename: Se Chan
authors.initials: SC
authors.lastname: Kang
authors.affiliation: Department of Chemistry, University of Ulsan, Ulsan 680-749, Republic of Korea. kwchi@ulsan.ac.kr.
authors.forename: Ki-Whan
authors.initials: KW
authors.lastname: Chi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D016207:Cytokines / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D004355:Drug Stability; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D016207:Cytokines; D008024:Ligands; D009942:Organometallic Compounds; D012428:Ruthenium; C031000:benzimidazole