Synthesis, characterization and biological activity of trans-platinum(II) complexes with chloroquine

Three platinum-chloroquine complexes, trans-Pt(CQDP)2(I)2 [1], trans-Pt(CQDP)2(Cl)2 [2] and trans-Pt(CQ)2(Cl)2 [3], were prepared and their most probable structure was established through a combination of spectroscopic analysis and density functional theory (DFT) calculations. Their interaction with DNA was studied and their activity against 6 tumor cell lines was evaluated. Compounds 1 and 2 interact with DNA primarily through electrostatic contacts and hydrogen bonding, with a minor contribution of a covalent interaction, while compound 3 binds to DNA predominantly in a covalent fashion, with weaker secondary electrostatic interactions and possibly hydrogen bonding, this complex also exerted greater cytotoxic activity against the tumor cell lines.

Graphical abstractThree trans- platinum-chloroquine complexes were prepared and characterized. Their interaction with DNA was studied and their activity against 6 tumor cell lines was evaluated. These complexes bind to DNA. All compounds exerted some degree of growth inhibition on the human tumor cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide