The Interaction of the Antitumor ComplexesNa[trans‐RuCl4(DMSO)(Im)] and Na[trans‐RuCl4(DMSO)(Ind)] WithApotransferrin: a Spectroscopic Study

Messori, Luigi; Kratz, Felix; Alessio, Enzo

doi:10.1155/mbd.1996.1

Cited by 55 publications

(35 citation statements)

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“…(areneϭp-cymene, hexamethylbenzene and lϭcarbene or nitrogen containing heterocycles) have been tested for antibacterial and antifungal activity.The tris chelates of the ruthenium with bidentate ligands show intercalate properties with the DNA 13) and bind to Fe(III) sites of the proteins lactoferin and transferrin 14,15) and transferrin is thought to be responsible for the delivery of Ru(III) to cancer cells where it is taken up via receptor mediated endocytosis.16) Transferrin normally transports Fe(III) in the blood but is only about one third occupied by Fe(III), and so there are vacant sites available for Ru(III) binding. Another important step in the mechanism of action of Ru(III) complexes is thought to be in vivo reduction to Ru(II), 17) which is kinetically more reactive than Ru(III).…”

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“…The tris chelates of the ruthenium with bidentate ligands show intercalate properties with the DNA 13) and bind to Fe(III) sites of the proteins lactoferin and transferrin 14,15) and transferrin is thought to be responsible for the delivery of Ru(III) to cancer cells where it is taken up via receptor mediated endocytosis. 16) Transferrin normally transports Fe(III) in the blood but is only about one third occupied by Fe(III), and so there are vacant sites available for Ru(III) binding.…”

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Synthesis, Anticancer and Antibacterial Activity of Some Novel Mononuclear Ru(II) Complexes

Mazumder

Gupta

Karki

et al. 2004

CHEMICAL & PHARMACEUTICAL BULLETIN

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The success of cisplatin and related platinum complexes as anticancer agents has stimulated a search for other active transition metal complexes, and ruthenium in particular has attracted the researchers.1) Metal complexes of ruthenium containing nitrogen and oxygen donor ligands are found to be effective catalysts for oxidation, reduction, hydrolysis and other organic transformation.2) The coordination environment around ruthenium plays the key role in stabilizing its different oxidation states and hence dictates the redox properties of the control atoms. (areneϭp-cymene, hexamethylbenzene and lϭcarbene or nitrogen containing heterocycles) have been tested for antibacterial and antifungal activity.The tris chelates of the ruthenium with bidentate ligands show intercalate properties with the DNA 13) and bind to Fe(III) sites of the proteins lactoferin and transferrin 14,15) and transferrin is thought to be responsible for the delivery of Ru(III) to cancer cells where it is taken up via receptor mediated endocytosis.16) Transferrin normally transports Fe(III) in the blood but is only about one third occupied by Fe(III), and so there are vacant sites available for Ru(III) binding. Another important step in the mechanism of action of Ru(III) complexes is thought to be in vivo reduction to Ru(II), 17) which is kinetically more reactive than Ru(III). Recently we have reported, N-alkyl and N-aryl substituted thiosemicarbazide complexes with Ru(bpy) 2 Cl 2 and greater antibacterial activity was found in the N-alkyl substituted complexes whereas N-aryl substituted exhibited more antitumor activity.18) In view of the above facts we have investigated the design of a novel range of Ru(II) complexes and the structural features as well as the contribution of the ligands that are responsible for antitumor and antibacterial activity. Results and DiscussionChemistry The ligands nmit (nmitϭN-methyl-isatin-3-thiosemicarbazone) and icpl (icplϭisatin-3-(4-chlorophenyl) thiosemicarbazone) were prepared by reacting Nmethylisatin and isatin with thiosemicarbazide and 4-chlorophenyl thiosemicarbazide in alcohol in presence of glacial acetic acid in 1 : 1 molar ratios respectively. Other ligands like r-tsc (r-tscϭ4-substituted thiosemicarbazides) were prepared according to the literature 19,20) with slight modification (Chart 1). All these ligands were confirmed for their purity by their melting point, elemental analysis and infrared spectra.Ruthenium metal complexes with the ligands nmit, icpl, aze (azeϭacetazolamide) and r-tsc were prepared by the reaction of a stoichiometric quantity of Ru(phen) 2 Cl 2 / Ru(bpy) 2 Cl 2 with the respective ligands in alcohol in presence of nitrogen (Chart 2). The completion of the reaction was monitored by TLC on silica gel.The structures of these ligands, especially nmit, icpl and rtsc in Fig. 1, show that in no case these ligands can exhibit tridentate behavior. There are very few cases in which the thiosemicarbazides act as monodentate ligands binding to the metal centre through the sulfur atom, th...

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Synthesis, Anticancer and Antibacterial Activity of Some Novel Mononuclear Ru(II) Complexes

Mazumder

Gupta

Karki

et al. 2004

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Transferrin is a 80 kDa blood plasma protein that transports iron into the cello As rapidly growing tumor tissues have a considerable need for iron, tumor cells have an increased amount of transferrin receptors on the cell surface. Radiolabelling experiments with 103Ru demonstrated an accumulation of a Ru(III)-transferrin adduct in the tumor of mice bearing subcutaneous EMT-6 sarcoma [171] [172],have been shown to bind to transferrin, specifically at the iron-binding defts, but also at histidine residues on the surface ofthe protein [173,174]. The transferrin-bound form ofthese complexes, prepared by preincubation with the protein, were tested in a human colon cancer cellline.…”

Section: Rutheniummentioning

confidence: 99%

Non-Platinum Antitumor Compounds

Pieper

Borsky

Keppler

1999

Metallopharmaceuticals I

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Non-platinum antitumor compounds have gained increasing interest during the last decade. A variety of antitumor active agents, from early transition to main -group metal or metalloid compounds, has been found and evaluated. Due to their different chemical characteristics, the mode of action and spectrum of activity of these compounds differ from each other. Antitumor activity in vitro is known for many compounds. Some compounds, like the ruthenium complexes, also exhibit promising in vivo activity. Two early transition metal complexes show interesting activity especially in experimental colon tumor models and are under evaluation in clinical trials: titanocene dichloride and budotitane. The two germanium complexes spirogermanium and germanium-132 have been evaluated but, despite their moderate toxicity, no encouraging results have been obtained. Gallium nitrate and gallium chloride are active against lymphomas and bladder cancer, and show a positive effeet on hypocalcaemias caused by tumors. They have undergone a number of clinical trials and are being investigated in promising combination regimens. Arsenic trioxide was found to be active against a rare blood cancer in clinical studies in China.

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“…In vitro and in vivo studies show high anticancer activity of ruthenium complexes and some of them are currently undergoing clinical trials [13,14]. It has been reported that trans- [HIm][Ru(III)Cl 4 (DMSO)(Im)] (NAMI-A) is active against tumor metastases, although this compound has a low cytotoxicity against cancer cells [15,16]. Ru(II) complexes coordinated by arene ligands also exhibit promising anticancer activity [17][18][19][20], thought to be due to the hydrophobic arene ligand which enhances the biomolecular recognition processes and transport of ruthenium through cell membranes.…”

Section: Introductionmentioning

confidence: 99%

Studies on cytotoxic and DNA-binding properties of two ruthenium(II) complexes of a substituted phenanthroline ligand

Mei

Wang

Liu

et al. 2008

Transition Met Chem

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Two chair ruthenium(II) complexes, K-and D-[Ru(bpy) 2 tFMPIP] 2 + (bpy = bipyridyl; tFMPIP = (2 0 -trifluoromethylphenyl)-imidazo-[4,5-f]-[1, 10]-phenanthroline, K-1 and D-1) have been synthesized and characterized by elemental analysis, ESI-MS and 1 H-NMR. The cytotoxicity of these complexes against human hepatocarcinoma cell line Bel-7402, human intestinal adenocarcinoma cell line HCT-8, and Human lung adenocarcinoma epithelial cell line A-549 have been investigated by colorimetric MTT (3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyl-1H-tetrazolium bromide) assay. Both K-1 and D-1 exhibit excellent inhibitory activity against the growth of Bel-7402 and HCT-8 cells. At dosage of 5 lg/cm 3 , the inhibition of K-1 and D-1 against human hepatocarcinoma cell line Bel-7402 is 85 and 85%, respectively. The studies on the DNAbinding properties of these complexes with Bel-7402 cell DNA by electronic spectra and steady state emission spectra, as well as circular dichlorism spectra show that there are detectable but subtle differences between K-1 and D-1, indicating the antitumor activity of these complexes is related to their DNA-binding behaviors.

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The Interaction of the Antitumor ComplexesNa[trans‐RuCl₄(DMSO)(Im)] and Na[trans‐RuCl₄(DMSO)(Ind)] WithApotransferrin: a Spectroscopic Study

Cited by 55 publications

References 2 publications

Synthesis, Anticancer and Antibacterial Activity of Some Novel Mononuclear Ru(II) Complexes

Synthesis, Anticancer and Antibacterial Activity of Some Novel Mononuclear Ru(II) Complexes

Non-Platinum Antitumor Compounds

Studies on cytotoxic and DNA-binding properties of two ruthenium(II) complexes of a substituted phenanthroline ligand

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