Book of Abstracts - Ruhr-Universität Bochum

P-52
ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum
Encapsulation of Pyrenyl-Containing Dendrimers in
Arene-Ruthenium Metalla-Prisms
A. Pitto-Barry, a N. Barry, a R. Deschenaux, a* and B. Therrien a *
a Université de Neuchâtel, Institut de chimie, 51 Ave de Bellevaux, 2000, Neuchâtel, Switzerland.
E-mail: bruno.therrien@unine.ch
Extravasation of macromolecules is considerably enhanced in tumor tissues. This phenomenon called
“enhanced permeability and retention” (EPR) effect is believed to play a major role in selective
delivery of nanomedicines. 1 Nanomedicines lead up to 100 times greater intratumor drug delivery
efficacy to cancer cells as compared to healthy cells. 2 Nanomedicines include antibodies and
polymeric drug but also large drug delivery vectors like micelles, nanoparticles and dendrimers.
Among new large drug carriers, we recently proposed to use metalla-prisms built from areneruthenium
units. 3 These water-soluble and cytotoxic metalla-assemblies offer many possibilities.
On the other hand, we have been working on dendritic system incorporating lipophilic functionalized
pyrenes. Encapsulation of the pyrenyl moiety in the hydrophobic cavity of the arene-ruthenium
metalla-prism, with the dendritic part hanging out of the cage, generates a potential target seeking
missile for cancer cells. The synthesis and characterization as well as the preliminary cytotoxicity
studies are presented.
References
1. Y. Matsumura, H. Maeda, Cancer Res. 1986, 46, 6387-6392.
2. H. Maeda, Adv Drug Deliv Rev. 2001, 46, 169-185.
3. B. Therrien, G. Süss-Fink, P. Govindaswamy, A. K. Renfrew, P. J. Dyson, Angew. Chem. Int. Ed.
2008, 47, 3773-3776.
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