NDLI: Ruthenium(II) arene PTA (RAPTA) complexes: impact of enantiomerically pure chiral ligands

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Dyson, Paul J. Cammack, Shona M. Clavel, Catherine M. Kilpin, Kelly J.
Description	Author Affiliation: Kilpin KJ ( Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.)
Abstract	Organometallic ruthenium(II) arene complexes containing the PTA ligand $([Ru(η^{6}-arene)Cl_{2}(PTA)],$ PTA = 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decane, termed RAPTA) show pharmacologically relevant anti-tumour properties in vitro. Two new enantiomeric pairs of RAPTA compounds, containing the chiral arene (R)- or (S)-2-phenyl-N-(1-phenylethylene)acetamide and either dichlorido or oxalato ligands were synthesised and fully characterised. The stability of the complexes towards hydrolysis was assessed and the dichlorido complexes were found to be more stable towards hydrolysis than the prototype complex RAPTA-C, $([Ru(η^{6}-p-cymene)Cl_{2}(PTA)]).$ The cytotoxicity of the compounds towards human ovarian cancer cells is moderate to good with a degree of selectivity towards the cancer cells over healthy cells. More significantly, for the first time we were able to establish the influence of a bulky, chiral group attached to the arene on the cytotoxicity of this class of compound, with the S-enantiomer being more cytotoxic than the R-enantiomer.
ISSN	14779226
Issue Number	6
Volume Number	42
e-ISSN	13645447
Journal	Dalton Trans.
Language	English
Publisher	Royal Society of Chemistry
Publisher Date	2013-02-14
Publisher Place	Great Britain (UK)
Access Restriction	Subscribed
Subject Keyword	Antineoplastic Agents Chemistry Coordination Complexes Organometallic Compounds Chemical Synthesis Toxicity Cell Line, Tumor Cell Survival Drug Effects Drug Resistance, Neoplasm HEK293 Cells Humans Hydrolysis Ligands Stereoisomerism Journal Article Research Support, Non-U.S. Gov't
Content Type	Text
Resource Type	Article
Subject	Inorganic Chemistry

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