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Book of Abstracts - Ruhr-Universität Bochum

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OP-18<br />

ISBOMC `10 5.7 – 9.7. 2010 <strong>Ruhr</strong>-<strong>Universität</strong> <strong>Bochum</strong><br />

Organometallic Anticancer Drugs: From Simple Structures to Rational Drug<br />

Design Based on a Mechanistic Approach<br />

Paul J. Dyson<br />

Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH<br />

1015 Lausanne, Switzerland. E-mail: paul.dyson@epfl.ch<br />

Organometallic chemistry has a strong tradition in the rational synthesis <strong>of</strong> compounds with<br />

specific functions, whatever the nature <strong>of</strong> the required function. But how is rational synthesis<br />

<strong>of</strong> organometallic pharmaceutical compounds currently achieved? The first part <strong>of</strong> the<br />

presentation will discuss the relevant issues by considering examples from the literature as<br />

well as from my own laboratory. 1 The presentation then continue with a focus on<br />

organometallic compounds based on the ruthenium(II)-arene unit developed in my laboratory<br />

that exhibit excellent in vivo anticancer activity and overcome certain limitations <strong>of</strong> presently<br />

used drugs. 2 The elements <strong>of</strong> the drug design process and the relevant known drug targets will<br />

be discussed. It will be shown that ligands with specific functions can be introduced into the<br />

drug structure in order to endow the compound with specific properties allowing the metal to<br />

perform a more classical role.<br />

One <strong>of</strong> the overriding features <strong>of</strong> the compounds discussed during the presentation is that<br />

targets other than DNA, i.e. enzyme and protein targets, are crucial for metal drugs, especially<br />

for the ruthenium(II)-arene drugs emanating from my laboratory, and evidence to support this<br />

notion will be provided.<br />

References<br />

1. C. G. Hartinger, P. J. Dyson, Chem. Soc. Rev., 2009, 38, 391–401.<br />

2. W. H. Ang, L. J. Parker, A. De Luca, L. Juillerat-Jeanneret, C. J. Morton, M. Lo Bello, M. W.<br />

Parker, P. J. Dyson, Angew. Chem. Int. Ed., 2009, 48, 3854–3857.<br />

34

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