ISBN: 978-83-60043-10-3 - eurobic9

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Eurobic9, 2-6 September, 2008, Wrocław, Poland KL5. Design and Mechanism of Reaction of Metal-Based Antitumor Agents and Artificial Metallonucleases Z. Guo Chemistry, Nanjing University, Hankou Road, No. 22, 2<strong>10</strong>093, Nanjing, China, e-mail: zguo@nju.edu.cn The side effects of the current clinic drugs have stimulated the research on the novel platinum-based antitumor complexes. Improving the tumor-selectivity of these complexes may mitigate the toxic effects and enhance the therapeutic index of these drugs. Design of complexes with novel structural features is another major focus of the area. In this talk, a strategy that can encapsulate Pt drugs in ferritin cage will be discussed. Conjugation of photodynamic therapeutic agent with cisplatin provides the possibility of red light excited cytoxicity of platinum-based compounds. Moreover, several new polynuclear Pt(II) complexes with robust structural features, designed in our lab, will be also discussed. These complexes have different structural features from cisplatin and have demonstrated notable cytotoxic activity against tumour cell lines. Their reactivity towards DNA and GSH has been investigated. Selective cleavage of DNA is of paramount interests in medicine and biotechnology. Transition metal complexes stand out as candidates for artificial nucleases due to their diverse structural features and reactivities. We have designed and structurally characterized a series of polynuclear copper and zinc complexes and studied their cleavage activity towards DNA and DNA model compounds. Structural factors that determine the activity will be discussed. References: [1] Yang, Z.; Wang, X.; Diao, H.; Zhang, J. Li, H.; Sun, H.; Guo, Z.J. Chem. Commun. 2007, 3409. [2] Wang, X.Y.; Guo Z.J., Dalton Trans., 2008, 1521. _____________________________________________________________________ 24
Eurobic9, 2-6 September, 2008, Wrocław, Poland KL6. Coupling Molecular Recognition and Signaling A. Shanzer, R. Kikkeri, G. Melman and Y. Barda Department of Organic Chemistry, Weizmann Institute of Science, P.O. Box 26, Rehovot, Israel Novel recognition-signaling conjugates, which integrate molecular recognition with signaling provides a powerful tool in the study of molecular recognition events in real time. Further improvements are obtained by combining spectroscopy and microscopy to generate dynamic probes to follow cellular events as they unfold. The generality of these conjugates will be demonstrated in following diverse events including: intracellular compartmentalization, molecular trafficking and identification of secondary targets. The limitations of using several probes simultaneously will be outlined and means to overcome these limitations by developing ‘tunable’ probes capable of emitting at different wavelength will be described. Advantages and limitations will be discussed. References: [1] R. Kikkeri, H. Traboulsi, N. Humbert, E. Gumienna-Kontecka, R. Arad-Yellin, G. Melman, M. Elhabiri, A.M. Albrecht-Gary, A. Shanzer. Inorganic Chemistry 46, 2485 (2007). _____________________________________________________________________ 25
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ISBN: 978-83-60043-10-3 - eurobic9

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