title: Self-assembled supramolecular hetero-bimetallacycles for anticancer potency by intracellular release.
abstract: Two new tetracationic hetero-bimetallacycles, compounds 4 and 5, have been constructed from an N,N'-bis(4-(pyridin-4-ylethynyl)phenyl)pyridine-2,6-dicarboxamide ligand (1), and cis-blocked complexes [M(dppf)(OTf)2 ] (dppf=1,1'-bis(diphenylphosphino)ferrocene; OTf=trifluoromethanesulfonate; M=Pd (2), Pt (3)) in CH3 NO2 /CH2 Cl2 (1:1) solvent. Both complexes were isolated with adequate yields as triflate salts and were then characterized using (1) H, (13) C, and (31) P NMR spectroscopy, elemental analysis, UV/Vis spectroscopy, and high-resolution electrospray mass spectrometry (HR-ESMS). The molecular structure of 4 was determined by molecular mechanics force-field calculations. The cytotoxic effect of both new complexes were analyzed against T98G (brain tumor), KB (head and neck cancer), SNU-80 (thyroid cancer), and HEK-293 non-malignant cell lines. The cytotoxicity of complexes 4 and 5 were found to be considerably more effective against cancer cells than reference drug cisplatin. Annexin-V/PI staining, caspase-3/7 activity, and the reduction in mitochondrial membrane potential justify a significant level of apoptosis in complex-treated cells.
authors.affiliation: Department of Chemistry, University of Ulsan, Ulsan 680-749 (Republic of Korea).
authors.forename: Anurag
authors.initials: A
authors.lastname: Mishra
authors.forename: Seung
authors.initials: S
authors.lastname: Chang Lee
authors.forename: Neha
authors.initials: N
authors.lastname: Kaushik
authors.forename: Timothy R
authors.initials: TR
authors.lastname: Cook
authors.forename: Eun Ha
authors.initials: EH
authors.lastname: Choi
authors.forename: Nagendra
authors.initials: N
authors.lastname: Kumar Kaushik
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Stang
authors.forename: Ki-Whan
authors.initials: KW
authors.lastname: Chi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D057809:HEK293 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D009369:Neoplasms / Q000188:drug therapy; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010165:Palladium / Q000737:chemistry*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D009944:Organoplatinum Compounds; D011725:Pyridines; D010165:Palladium
keywords: antitumor agents; biological activity; ligands; metallacycles; self-assembly; supramolecular chemistry