This work highlights possible new coordination metal drugs for the treatment of cancer. Unlike other coordination complexes which have shown issues with drug formulation, we present new metal complexes which are stable as single isomers with nanomolar potencies. This is contrary to earlier literature which considered trans-Pt complexes to be inactive due to high kinetic instability. A library of bis-picolinamide platinum-based metal(III) dihalide complexes have been synthesised, MX2L(LH) (M = Ru or Rh, X = Cl or I and L = picolinamide) and structural studies revealed a mixture of cis and trans isomers for the MCl2L(LH) complexes. Changing the halide to iodide, MI2L(LH), exclusively generates a single trans isomer. Chemosensitivity studies show high cytotoxic activity against human cancer cell lines, with potencies for selected complexes similar to or better than cisplatin. The MI2L(LH) complexes show a substantial increase in cytotoxicity when compared to the MCl2L(LH) complexes, with selectivity against human colorectal cancers (Fig. 1). The data against healthy cells, hypoxic assays and hydrolysis studies are also discussed. Conclusively, the change in conformers from cis to trans triggers high in vitro activity, cancer cell selectivity and the complexes remain active under hypoxic conditions. The results highlight these complexes as excellent candidates for further in vivo studies.

Ruthenium(III) and rhodium(III) dihalide complexes: Showing high potency and cancer cell selectivity for trans isomers

256th National Meeting (2018)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.