Titel
{Ru(CO)x}-Core complexes with benzimidazole ligands: synthesis, X-ray structure and evaluation of anticancer activity in vivo
Autor*in
Gabriella Tamasi
Department of Biotechnology, Chemistry and Pharmacy, University of Siena
Autor*in
Antonello Merlino
Department of Chemical Sciences, University of Naples Federico II
Autor*in
Federica Scaletti
Department of Chemistry, University of Florence
... show all
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.
Objekt-Typ
Sprache
Englisch [eng]
Persistent identifier
https://phaidra.univie.ac.at/o:561660
Erschienen in
Titel
Dalton Transactions
Band
46
Ausgabe
9
Seitenanfang
3025
Seitenende
3040
Verlag
Royal Society of Chemistry (RSC)
Erscheinungsdatum
2017
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