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Adding diversity to ruthenium(II)–arene anticancer (RAPTA) compounds via click chemistry: The influence of hydrophobic chains

Year: 2011

Journal: Journal of Organometallic Chemistry, Volume 696, Issue 3, 1 February 2011, Pages 772-779, 20111221

Authors: Anna K. Renfrew a , Lucienne Juillerat-Jeanneret b , Paul J. Dyson a, *

Organizations: a Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland, b Institute of Pathology, University Hospital (CHUV), University of Lausanne, Lausanne, Switzerland

The application of click chemistry to develop libraries of organometallic ruthenium–arene complexes with potential anticancer properties has been investigated. A series of ruthenium–imidazole–triazole complexes, with hydrophobic tails, were prepared from a common precursor via click chemistry. The tail could be attached to the ligand prior to coordination to the ruthenium complex or following coordination, the former giving the product in superior yield. The complexes were screened for cytotoxicity in tumourigenic and non-tumourigenic cell lines, and while the compounds were only moderately cytotoxic, good selectivity for tumourigenic cells was observed.