Regresar

A new complex of copper-phosphole. Synthesis, characterization and evaluation of biological activity

Abstract:

As part of the search for effective cancer chemotherapy, we describe here the synthesis, characterization, structural determination and biological activity of a new copper complex [Cu{1-phenyl-2,5-bis(2-thienyl)phosphole}2Cl] (1), and evaluated its biological activity in terms of binding to calf thymus (CT) DNA, distribution coefficient, interaction with thioredoxin reductase (TrxR) and inhibition of tumour cell lines. Spectroscopic titration and viscosity results suggested a noncovalent interaction with DNA, probably by π–π stacking or electrostatic, while electrophoresis and competitive studies showed a weak interaction with CT-DNA. On the other hand, the TrxR system does not seem to be a target of action and the lipophilicity of the compound indicates that it may penetrate the cell membrane more effectively than the ligand or cisplatin. Finally, the compound showed little inhibitory effect on the tumour cell lines. With these results, we proposed that the low activity of the compound is due to only weak interaction with specific targets such as DNA.