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Issue 9, 2017
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{Ru(CO)x}-Core complexes with benzimidazole ligands: synthesis, X-ray structure and evaluation of anticancer activity in vivo

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Abstract

The reaction of [RuII2(CO)6Cl2], 1, with [N with combining low line]3-methylbenzimidazole (MBI) and 5,6-dimethylbenzimidazole (DMBI) afforded two new complexes with the general formula fac-[RuII(CO)3Cl2L], L = MBI (2) or DMBI (4). Crystals of cis,trans-[RuII(CO)2Cl2([N with combining low line]3-MBI)2], 3, were also obtained from the mother liquor that produced 2. In the presence of water, the dissociation of Ru–N, Ru–Cl and Ru–CO bonds occurred as a function of time, water content and pH. Density functional theory structure simulations/optimizations were carried out at the Becke3LYP level of theory for evaluating the relative stability of possible conformers. ESI-MS studies revealed the ability of the complexes to link model proteins, such as lysozyme, bovine pancreatic ribonuclease and cytochrome c, with the partial release of the heteroaromatic base, chlorido and carbonyl ligands. X-ray diffraction studies on crystals grown from a solution of HEWL and 2 showed the partial removal of chloride and CO. Cytotoxicity tests yielded two-digit micromolar IC50 values in CH1/PA-1 and SW480 cancer cells. In contrast to CORM-3 and 2, a significantly reduced tumor growth was observed with 4 in the murine colon cancer CT-26 model in vivo.

Graphical abstract: {Ru(CO)x}-Core complexes with benzimidazole ligands: synthesis, X-ray structure and evaluation of anticancer activity in vivo

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Publication details

The article was received on 11 Nov 2016, accepted on 03 Feb 2017 and first published on 16 Feb 2017


Article type: Paper
DOI: 10.1039/C6DT04295C
Citation: Dalton Trans., 2017,46, 3025-3040
  • Open access: Creative Commons BY license
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    {Ru(CO)x}-Core complexes with benzimidazole ligands: synthesis, X-ray structure and evaluation of anticancer activity in vivo

    G. Tamasi, A. Merlino, F. Scaletti, P. Heffeter, A. A. Legin, M. A. Jakupec, W. Berger, L. Messori, B. K. Keppler and R. Cini, Dalton Trans., 2017, 46, 3025
    DOI: 10.1039/C6DT04295C

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