Abstract

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.

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