title: Photoluminescent DNA binding and cytotoxic activity of a platinum(II) complex bearing a tetradentate β-diketiminate ligand.
abstract: A platinum(II) complex of a monoanionic, tetradentate β-diketiminate (BDI) ligand with pendant quinoline arms, BDI(QQ)H, is reported. The complex, [Pt(BDI(QQ))]Cl, is emissive in DMSO, but non-emissive in aqueous buffer. Upon binding DNA in buffer, however, a 150-fold turn-on in emission intensity occurs. Dynamic light scattering and (1)H NMR spectroscopy indicate that [Pt(BDI(QQ))]Cl forms non-emissive aggregates in aqueous solution; DNA-binding disperses the aggregates leading to the large emission turn-on response. The cytotoxic activity of the complex, measured in two cancer cell lines, is comparable to or better than that of the established anticancer drug cisplatin.
authors.affiliation: Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Hope
authors.forename: Justin J
authors.initials: JJ
authors.lastname: Wilson
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Lippard
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D007097:Imines / Q000737:chemistry*; D008024:Ligands; D008027:Light; D008958:Models, Molecular; D008968:Molecular Conformation; D009570:Nitriles / Q000737:chemistry*; D009944:Organoplatinum Compounds / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D007097:Imines; D008024:Ligands; D009570:Nitriles; D009944:Organoplatinum Compounds; C542835:ketimine; D004247:DNA