Book of Abstracts - Ruhr-Universität Bochum

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OP-19 ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum Biological Activity of Gold and Silver Bis(Phosphino)Hydrazine Complexes Frederik H. Kriel, *a and Judy Coates a a AuTEK Biomed, Mintek, Private Bag X3015, Randburg, 2125, South Africa. E-mail: erikk@mintek.co.za The anti-tumour potential of gold(I) phosphine complexes was first identified at the time when auranofin was shown to kill tumour cells in culture. This sparked the interest of Berners-Price et al. 1,2 and led to the development of the bis-chelated gold(I) phosphine anti-tumour compound [Au(bis(diphenylphospino) ethane)2]Cl and later [Au(bis(di-2-pyridalphosphino)ethane)2]Cl. Clinical development of delocalised lipophilic cations has been hindered by severe toxicity, but several classes of these compounds have demonstrated a relationship between anti-tumour selectivity and lipophilichydrophilic balance. 1,2 Following on the work done by Berners-Price et al.; a series of hydrazine-bridged ligands have been synthesised to modulate the lipophilic-hydrophilic balance of the resulting complexes. 3,4 These include the phenyl, p-methoxyphenyl and p-dimethylaminophenyl derivatives of the bis-phosphine. The main focus of the research is on the group 11 transition metals and corresponding gold and silver phosphine complexes. Here we describe the anti-tumour activity and NCI 60 cell line profile of these compounds. Acknowledgements The authors would like to thank the University of Pretoria for use of their facilities. Prof. Connie Medlen, Dr. Gisella Joone and Mrs. Margo Nell for guidance. Prof. Denver Hendricks at the University of Cape Town for reviewing the work. National Research Fund for the funding for training. The NCI for the 60 cell line screen. AuTEK Biomed (Mintek and Harmony) for permission to publish the results and financial support. References 1 S. J. Berners-Price, Chem. Aust., 2004, 71, 10. 2 S. J. Berners-Price, P. J. Sadler, Struc. and Bond., 1988, 70, 27. 3 V. S. Reddy, K. V. Katti, Inorg. Chem., 1994, 33, 2695. 4 F. H. Kriel, M. Layh, H. M. Marques, J Coates, Ph.D. Thesis, University of the Witwatersrand, 2007. 35
OP-20 ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum DNA and Protein Binding, Cleavage and Anticancer Activity of Organometallic (M = Ru(II), Rh(III) and Ir(III)) Arene Complexes R. Loganathan, a S. Ramakrishnan, a P. Kumar, c D. S. Pandey, c A. Riyasdeen, b M. A. Akbarsha, b and Mallayan Palaniandavar* a a Centre for Bioinorganic Chemistry, School of Chemistry, b Department of Animal Science, Bharathidasan University, Tiruchirapalli 620 024, India. c Department of Chemistry, Facult of Science, Banaras Hindu University, Varanasi 221 005, India. E-mail: palanim51@yahoo.com The study of organometallic compounds as anticancer agents is receiving much attention now. These compounds can be tuned by using suitable chelating ligands to facilitate their uptake into the cells or for selectivity of reactions with DNA or proteins. However, the number of such studies is very limited. This is because of the low solubility and instability in water and poor uptake by the cells. The ruthenium complexes NAMI-A and KP1019, which show prominent anticancer activity, are currently in clinical trials for the treatment of metastasis and colorectal cancers, respectively. Very recently, we have shown that non-covalent interactions of certain water soluble Ru(II) complexes 1,2 with DNA enhances the cytotoxicity against several cancer cell lines. It is noteworthy that a family of ruthenium(II)–arene complexes developed by Sadler, and Dyson et al. exhibits high in vitro and in vivo anticancer activity. The titanocene dichloride has already completed phase II clinical trials and ferrocifen, which is a ferrocenyl derivative of tamoxifen, appears set to enter clinical trials soon. More recently, increasing interest has been focused on organometallic-arene compounds, which show excellent antiproliferative properties in vitro and in vivo. In this work a series of water soluble organometallic complexes of the type [{Ru(η 6 -arene)(L)Cl}](BF4)2 (arene = benzene; 1 and p-cymene; 2) and [{(η 5 - C10Me5)M(L)Cl}](BF4)2, (M = Rh; 3 and Ir; 4 and L = benzyl-di-pyridin-2-yl-amine) has been isolated and the structures of 3 and 4 have been determined by X-ray crystallography. The bidentate benzyl-di-pyridin-2-ylamine ligand is designed to provide hydrophobicity. Also, the present compounds are equipped with a chloride leaving group in order to enable covalent interaction of the complexes with biological targets. Further, the arene ligand provides hydrophobicity thus tuning the DNA- and protein-binding and DNA- and protein-cleaving properties of the complexes. The interactions of these metal complexes with CT DNA have been explored by using absorption, emission and CD spectroscopy and electrochemical and viscosity measurements. DNA and protein cleavage reactions have also been studied using agarose and polyacrylamide gel electrophoresis respectively. The anticancer activities and the mode of cell death have also been established. The results of our systematic investigations will be presented and discussed. References N3 N2 N1 Cl Rh 1. V. Rajendiran, M. Murali, E. Suresh, S. Sinha, K. Somasundaram, M. Palaniandavar Dalton Trans. 2008, 148-163. 2. V. Rajendiran, M. Murali, E. Suresh, M. Palaniandavar, V.S. Periasamy, M.A. Akbarsha Dalton Trans. 2008, 2157-2170. 36 N3 N2 N1 Cl Ir
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Sergey Abramkin Universität Wien,
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Prof. Dr. Toshikazu Hirao Osaka Uni
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Book of Abstracts - Ruhr-Universität Bochum

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