Aminophosphine ligands as a privileged platform for development of antitumoral ruthenium(<scp>ii</scp>) arene complexes

L.M. Broomfield, Carlos Alonso‐Moreno, Eddy Martín, Alexandr Shafir, Inmaculada Posadas, Valentı́n Ceña, José A. Castro‐Osma

Dalton Transactions · 2017 · 34 citations · 59 references

Concepts

Abstract

value range as low as 10-0.8 μM. Several biological assays were carried out to gain insight into the mechanism of action. Cell death by apoptosis and pH-independent action has been demonstrated. In addition, a selective cytotoxicity profile for tumoral cells over non-tumoral cells has been identified. Importantly, for the key candidates no loss of activity was observed when applied to the Pt-resistant A2780R, which highlights the potential utility of the bis-phospinoamine scaffold as an easily-tunable auxiliary ligand core in both drug discovery and subsequently a logical design of new anticancer metal-containing drugs. The complexes are characterised by NMR spectroscopy, mass spectrometry and single-crystal X-ray diffraction.

References

59