In vitro antitumor activity of water-soluble copper(I) complexes with diimine and monodentate phosphine ligands

Copper(I) complexes including diimine ligands of the bicinchoninic acid (BCA) and bathocuproinedisulfonic acid (BCS) families and water-soluble phosphines have been synthetized, characterized and investigated for their in vitro anticancer potential against human tumor cell lines representing examples of lung, breast, pancreatic and colon cancers and melanoma. All copper complexes exhibited moderate to high cytotoxic activity and the ability to overcome cisplatin resistance. Remarkably, growth-inhibitory effects evaluated in human non-transformed cells revealed a preferential cytotoxicity versus neoplastic cells. The remarkable cytotoxic effect towards BxPC3 pancreatic cancer cells, notoriously poor sensitive to cisplatin, was not related to a DNA or proteasome damage.