Anticancer Metallodrug Development: Novel Methods to Elucidate Modes of Action and in Pharmacophore Design
Since the discovery of cisplatin, a wide variety of metal complexes have been designed for the treatment of cancer and other diseases as well as for diagnostic purposes. Bioorganometallic chemistry is a thriving field of research and in particular the development of anticancer drugs based on organometallic moieties has received a lot of attention in recent years.1 The modes of action of anticancer metallodrugs are crucially dependent on their interactions with biological molecules.
As many established chemotherapeutics have low selectivity for tumor tissue, they cause adverse effects, which limit the dose that can be administered. Therefore, we are aiming for the development of targeted and targeting drugs, using organometallic fragments to interact selectively with a biomolecular target or to be selectively transported to and accumulated in tumor tissue.1 A brief overview of my groups recent contributions to the field of anticancer bioorganometallics will be given in this lecture, including important advances in our understanding of the modes of action to support future drug design. This presentation will focus on novel metal-based pharmacophores and the application of novel bioanalytical methods and their development, and the translation of these methods to identify new metal-based anticancer agents with promising biological properties .