Design, synthesis, characterization and biological studies of ruthenium and gold compounds with anticancer properties

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Design, synthesis, characterization and biological studies of ruthenium and gold compounds with anticancer properties

Type: Doctoral Thesis
Title: Design, synthesis, characterization and biological studies of ruthenium and gold compounds with anticancer properties
Author: Garza-Ortiz, Ariadna
Publisher: Leiden Institute of Chemistry, Faculty of Science, Leiden University
Issue Date: 2008-11-25
Keywords: Anticancer drugs
bis(arylimino)pyridine
Coordination compounds
Cyclization
Cytotoxicity
Gold
In-vitro studies
Infrared
NMR
Ruthenium
Stability studies
UV-Vis
X-ray difraction studies
2-(arylazo)pyridine
Abstract: The design of novel anticancer agents is one of the most active fields in Medicinal Chemistry, as the number of effective drugs for treatment of cancer is still very limited. This demand for new drugs is even higher, considering the high cancer-prevalence rate in our society. The therapeutic application of metal complexes is an under-developed area of research and basic principles in the development of metallopharmaceuticals are lacking, or at least just recently being discovered. Metal-containing agents may offer unique therapeutic opportunities. However, significant obstacles, including potential metal accumulations and toxicities, require further research before a promising metal compound may be introduced in the clinic. In particular several ruthenium and gold coordination compounds have shown promising application as anticancer agents. In these terms, this thesis project, performed in the Coordination and Bioinorganic Chemistry group in the Leiden Institute of Chemistry, comprises the design, synthesis, detailed characterization (i.e. elemental analysis, UV-Vis spectroscopy, IR, far-IR, NMR, mass spectroscopy and X-ray single-crystal structure determination) and also the biological evaluation of novel gold compounds and ruthenium compounds. The promising cytotoxic activity developed for several of these compounds and the findings from this research are providing a better understanding of chemistry of Ru(III) and Ru(II) and Au(III) coordination compounds and their structure-activity relationships and may lead to the development of improved ruthenium and gold-chemotherapeutic drugs.
Description: Promotor: J. Reedijk
With Summary in Dutch
Faculty: Faculteit der Wiskunde en Natuurwetenschappen
Citation: Garza-Ortiz, A., 2008, Doctoral thesis, Leiden University
Sponsor: Chemical Sciences of The Netherlands Organization for Scientific Research (CW-NWO), Consejo Nacional de Ciencia y Tecnologia (CONACyT), TEVA-Pharmachemie, European Cooperation in the Field of Scientific and Technical Research (COST), Johnson and Matthey (Reading, UK), Leiden Institute of Chemistry, Leiden University
Handle: http://hdl.handle.net/1887/13280
 

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application/pdf Title page 892.0Kb View/Open
application/pdf Table of conten ... viations_List of chemicals 841.8Kb View/Open
application/pdf Chapter 1 1.464Mb View/Open
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application/pdf Chapter 5 1.959Mb View/Open
application/pdf Chapter 6 Summary_Conclusions and further remarks 655.4Kb View/Open
application/pdf Some extra data 932.3Kb View/Open
application/pdf Summary in Dutch 378.4Kb View/Open
application/pdf Curriculum Vitae 362.8Kb View/Open
application/pdf List of Publications 401.1Kb View/Open
application/pdf Acknowledgements 360.1Kb View/Open
application/pdf Back Cover 114.4Kb View/Open
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