title: Synthesis, characterization and biological activity of trans-platinum(II) complexes with chloroquine.
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.
authors: Centro de Química, Instituto Venezolano de Investigaciones Científicas (IVIC), Altos de Pipe, Caracas, Venezuela. mnavarro@ivic.gob.ve
authors: Maribel
authors: M
authors: Navarro
authors: William
authors: W
authors: Castro
authors: Angel R
authors: AR
authors: Higuera-Padilla
authors: Anibal
authors: A
authors: Sierraalta
authors: María Jesús
authors: MJ
authors: Abad
authors: Peter
authors: P
authors: Taylor
authors: Roberto A
authors: RA
authors: Sánchez-Delgado
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002614:Chelating Agents / Q000737:chemistry*; D002738:Chloroquine / Q000737:chemistry*; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D004247:DNA; D053837:DNA Cleavage; D004270:DNA, Circular / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D010984:Platinum
chemical_list: D000970:Antineoplastic Agents; D002614:Chelating Agents; D056831:Coordination Complexes; D004270:DNA, Circular; D010984:Platinum; D002738:Chloroquine; D004247:DNA; C427203:calf thymus DNA