The development of successful chemotherapeutics faces two main problems: acquired resistance to drugs and lack of selectivity of the drugs for tumor cells over normal cells. This has resulted in increasing interest in targeted drug design; for example, design of drugs that selectively target the mitochondria of tumour cells because of their pivotal role in apoptosis. Au(I) lipophilic cations are promising chemotherapeutic candidates in this regard, with growing evidence for their antimitochondrial mechanism of action [1, 2]. However, a deeper understanding of their function and sub-cellular localisation is needed. The availability of suitable imaging techniques to map the subcellular distribution of the drugs is therefore essential.