Book of Abstracts - Ruhr-Universität Bochum

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ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum
Novel Metallocene Anticancer Drugs: From Lead to Hit
Matthias Tacke a
a Centre for Synthesis and Chemical Biology, Conway Institute
UCD School of Chemistry and Chemical Biology, Belfield, Dublin 4, Ireland.
E-mail: matthias.tacke@ucd.ie
Titanocene dichloride derivatives like Titanocene Y were extensively investigated in vitro, in vivo
and ex vivo during the last years. 1-5 In addition, details about the mechanism of action became
available, which allowed for choosing renal-cell cancer as one of the appropriate targets. More
recently, the successful substitution patterns of the titanocenes were transmetallated onto vanadium
which has led to isostructural vanadocene dichloride compounds. 6, 7 These compounds have started
their preclinical evaluation process with respect to their cytotoxicity and anti-angiogenic activity in
vitro and their tumor volume control and toxicity in vivo. The results allow for the first to look at the
direct comparison of these two promising classes of metallocene compounds; this might allow to
answer the question, which metal is the most promising for further development.
References
1. Bioorganometallic Fulvene-Derived Titanocene Anticancer Drugs, K. Strohfeldt, M. Tacke, Chem.
Soc. Rev., 2008, 37, 1174-1187.
2. In Vitro Anti-Tumor Activity of Bridged and Unbridged Benzyl-Substituted Titanocenes, G. Kelter,
N. Sweeney, K. Strohfeldt, H.-H. Fiebig, M. Tacke, Anti-Cancer Drugs, 2005, 16, 1091-1098.
3. Antitumor Activity of Titanocene Y in Xenografted Caki-1 Tumors in Mice, I. Fichtner, C.
Pampillón, N. J. Sweeney, K. Strohfeldt, M. Tacke, Anti-Cancer Drugs, 2006, 17, 333-336.
4. Antitumor Activity of Titanocene Y in Freshly Explanted Human Breast Tumors and in Xenografted
MCF-7 Tumors in Mice, Anti-Cancer Drugs, 2007, 18, 311-315.
5. Antiproliferative Activity of Titanocene Y against Tumor Colony Forming Units, O. Oberschmidt,
A.-R. Hanauske, C. Pampillón, K. Strohfeldt, N. J. Sweeney, M. Tacke, Anti-Cancer Drugs, 2007, 18,
317-321.
6. Novel Benzyl-Substituted Vanadocene Anticancer Drugs, B. Gleeson, J. Claffey, M. Hogan, H.
Müller-Bunz, D. Wallis, M. Tacke, J. Organometal. Chem., 2009, 694, 1369-1374.
7. Synthesis and Cytotoxicity Studies of Fluorinated Derivatives of Vanadocene Y, B. Gleeson, J.
Claffey, A. Deally, M. Hogan, L. M. Menéndez Méndez, H. Müller-Bunz, S. Patil, D. Wallis, M.
Tacke, Eur. J. Inorg. Chem., 2009, 2804-2810.
Acknowledgement: Support is acknowledged from CESAR, COST, HEA, CSCB and UCD.
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