Publications de Claudine Scolaro

Importance of the p-Ligand: Remarkable Effect of the Cyclopentadienyl Ring on the Cytotoxicity of Ruthenium PTA Compounds

Paul Joseph Dyson, Rosario Scopelliti, Kay Severin, Claudine Scolaro, Barnali Dutta

The water-sol. complexes [(Cp'OR)RuCl(PTA)2] (Cp'OR = h5-1-alkoxy-2,4-di-tert-butyl-3-neopentylcyclopentadienyl; R = Me, Et; PTA = 1,3,5-triaza-7-phosphaadamantane) are considerably more cytotoxic (.apprx.2 orders of magnitude) than the cyclopentadienyl an ...

2008

Hydrolysis study of the bifunctional antitumor compound RAPTA-C, [Ru(η6-p-cymene)Cl2(pta)]

Paul Joseph Dyson, Christian Hartinger, Claire Samantha Allardyce, Claudine Scolaro

The hydrolysis of [Ru(η6-p-cymene)Cl2(PTA)] (PTA = 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decanephosphine; RAPTA-C) was studied using UV-visible (UV-vis) spectrophotometry and NMR spectroscopy. In analogy to in silico studies, [Ru(η6-p-cymene)Cl(H2O)(PTA) ...

2008

Tuning the hydrophobicity of ruthenium(II)-arene (RAPTA) drugs to modify uptake, biomolecular interactions and efficacy

Paul Joseph Dyson, Claudine Scolaro, Christian Hartinger, Gianni Sava

The antitumor activity of the organometallic ruthenium(II)-arene mixed phosphine complexes, [Ru(h6-p-cymene)Cl(PTA)(PPh3)]BF4 1b and [Ru(h6-C6H5CH2CH2OH)Cl(PTA)(PPh3)]BF4 2b (PTA = 1,3,5-triaza-7-phosphaadamantane), have been evaluated in vitro and compare ...

2007

Development of Ruthenium Antitumor Drugs that Overcome Multidrug Resistance Mechanisms

Paul Joseph Dyson, Rosario Scopelliti, Wee Han Ang, Andrew Douglas Phillips, Claudine Scolaro, Gianni Sava

Organometallic ruthenium(II) complexes of the general formula [Ru(η6-p-cymene)Cl2(L)] and [Ru(η6-p-cymene)Cl(L)2][BPh4] with modified phenoxazine- and anthracene-based multidrug resistanc ...

2007

Structure-activity relationships for ruthenium(II)-arene drugs : in vitro and in vivo antitumour evaluation

Claudine Scolaro

The discovery of the anticancer properties of cisplatin in 1965 heralded the development of metallopharmaceuticals and founded a revolution in cancer therapy. Platinum drugs are believed to induce cytotoxicity by cross-linking DNA, causing changes to the D ...

EPFL2007

Influence of Hydrogen-Bonding Substituents on the Cytotoxicity of RAPTA Compounds

Paul Joseph Dyson, Ursula Röthlisberger, Ivano Tavernelli, Christian Gossens, Claudine Scolaro, Sébastien Rochat, Antoine Dorcier, Gianni Sava

A new series of organometallic ruthenium(II)-arene compounds of the type RuCl2(η6-arene)(phosphine) (phosphine = 1,3,5-triaza-7-phosphaadamantane, PTA, and 3,7-diacetly-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane, DAPTA) with different ...

2006

Synthesis, Characterization, and in Vitro Evaluation of Novel Ruthenium(II) η6-Arene Imidazole Complexes

Paul Joseph Dyson, Rosario Scopelliti, Andrew Douglas Phillips, Claudine Scolaro, Gianni Sava

Ten complexes of general formula [Ru(η6-arene)Cl2(L)], [Ru(η6-arene)Cl(L)2][X], and [Ru(η6-arene)(L)3][X]2 (η6-arene = benzene, p-cymene; L = imidazole, ...

2006

Development of Organometallic Ruthenium-Arene Anticancer Drugs That Resist Hydrolysis

Paul Joseph Dyson, Rosario Scopelliti, Wee Han Ang, Elisa Daldini, Claudine Scolaro

With a view to develop drugs that could resist hydrolysis in aq. media,organometallic arene-capped ruthenium(II) 1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane (RAPTA) complexes bearing chelating carboxylate ligands have been prepd. and studied. The new com ...

2006

In vitro and in vivo evaluation of ruthenium(II)-arene PTA complexes

Paul Joseph Dyson, Gabor Laurenczy, Claudine Scolaro, Gianni Sava

The antitumor activity of the organometallic ruthenium(II)-arene complexes, RuCl2(eta(6)-arene)(PTA), (arene = p-cymene, toluene, benzene, benzo-15-crown-5, 1-ethylbenzene-2,3-dimethylimidazolium tetrafluoroborate, ethyl benzoate, hexamethylbenzene; PTA = ...

2005

Is the aromatic fragment of piano-stool ruthenium compounds an essential feature for anticancer activity? The development of new Ru-II-[9]aneS(3) analogues

Paul Joseph Dyson, Claudine Scolaro

New half-sandwich R-II-[9]aneS(3) complexes ([9]aneS(3) = 1,4,7-trithiacyclononane), namely [RuCl2(PTA)([9]aneS(3))] (4), [RuCl(PTA)(2)([9]aneS(3))][OTf] (5), [RuCl(en)([9]aneS(3))][OTf] (6), [RuCl(enac)([9]aneS(3))][OTf] (7), [RuCl(bipy)([9]ane-S-3)][OTf] ...

2005