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Project 3

Novel antineoplastic Pt(IV) complexes. Synthesis, characterization, biological investigations and SAR

Supervisor: Prof. Markus Galanski

Student: Hristo Varbanov

Cancer is the second most frequent cause of death in developed countries. Today, three platinum-based chemotherapeutics, namely cisplatin, carboplatin and oxaliplatin are in worldwide clinical use. These metal complexes are administered in nearly 50% of all anticancer therapies. In this context it is worthwhile mentioning that cisplatin is one of the few anticancer agents with curative potential in the case of testicular cancer. Cure rates of more than 90% are reached.

Nevertheless, platinum-based chemotherapy is accompanied by a set of severe side-effects. In addition, not all tumors are susceptible to these cytotoxic agents and therapy is often limited because of an acquired or intrinsic resistance of the tumor cells. In order to overcome these limitations, also octahedral configured platinum(IV) complexes such as satraplatin have been investigated in clinical trials. Satraplatin is kinetically inert and shows in comparison to the platinum(II) complexes an altered spectrum of systemic toxicity. Satraplatin was investigated in phase III clinical trials against hormone refractory prostate cancer.

The aim of the project is to develop novel platinum(IV) complexes. This includes the synthesis, an in depth characterization via elemental analysis, ESI-MS, IR, X-ray diffraction, and multinuclear (1H, 13C, 15N, 195Pt) NMR spectroscopy. Moreover, their cytotoxic and anticancer potential as well as their lipophilicity, cellular accumulation and redox potential will be investigated. In last consequence a lead structure should be found and structure-activity relationships should be optimized.

Initiativkolleg Functional Molecules
Währinger Str. 38
1090 Wien
T: +43 1 4277 70809
Universität Wien | Universitätsring 1 | 1010 Wien | T +43-1-4277-0