In vitro antitumor activity of the water soluble copper(I) complexes bearing the tris(hydroxymethyl)phosphine ligand.

摘要: Monocationic hydrophilic complexes [Cu(thp)4](+) 3 and [Cu(bhpe)2](+) 4 were synthesized by ligand exchange reactions starting from the labile [Cu(CH3CN)4][PF6] precursor in presence of an excess relevant phosphine. Complexes tested against a panel several human tumor cell lines. Complex has been shown to be about 1 order magnitude more cytotoxic than cisplatin. Chemosensitivity tests performed on cisplatin multidrug resistance phenotypes suggested that complex acts via different mechanism action reference drug. Different short-term proliferation assays lysosomal damage is early cellular event associated with cytotoxicity, probably mediated increased production reactive oxygen species. Cytological stains flow cytometric analyses indicated phosphine copper(I) able inhibit growth cells G2/M cycle arrest paraptosis accompanied loss mitochondrial transmembrane potential.