6533b858fe1ef96bd12b5987
RESEARCH PRODUCT
DNA Binding Studies and Cytotoxicity of a Dinuclear PtII Diazapyrenium- Based Metallo-supramolecular Rectangular Box
Michael J. HannonJosé M. QuintelaCosimo DucaniGiampaolo BaroneLenka ZerzankovaLenka ZerzankovaPatrick J. BednarskiAron F. WestendorfAlessio TerenziAlessio TerenziVíctor BlancoCarlos Peinadorsubject
Organoplatinum CompoundsCell SurvivalStereochemistryIntercalation (chemistry)Molecular ConformationSupramolecular chemistryAntineoplastic AgentsApoptosisLigandsNucleic Acid DenaturationLinear dichroismCatalysissupramolecular chemistryInhibitory Concentration 50chemistry.chemical_compoundCell Line TumorSettore BIO/10 - BiochimicaHumansmetallodrugPlatinumnoncovalent DNA bindingChemistryCircular DichroismOrganic ChemistryDNA NeoplasmGeneral ChemistrySettore CHIM/06 - Chimica OrganicaMetallacycleLigand (biochemistry)Binding constantFluorescenceSettore CHIM/08 - Chimica FarmaceuticaIntercalating AgentsKineticsSpectrometry FluorescenceSettore CHIM/03 - Chimica Generale E InorganicaThermodynamicscytotoxicityPtII rectangular boxCisplatinDNAPhenanthrolinesdescription
The interaction with native DNA of a 2,7-diazapyrenium-based ligand 1 and its Pt II rectangular metal- lacycle 2 is explored through circular and linear dichroism and fluorescence spectroscopies. The metal-free ligand 1 binds through intercalation, with a binding constant of approximately 5 � 10 5 m � 1 , whereas the metallacycle 2 binds and bends the DNA with a bind- ing constant of 7 � 10 6 m � 1 . PCR assays show that metallo-supramolecular box 2 interferes with DNA transactions in vitro whereas the intercalator 1 does not. The metallacycle is active against four human cancer cell lines, with IC50 values ranging between 3.1 and 19.2 mm and shows similar levels of efficacy, but a different spectrum of activity, to cis- platin.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2012-07-16 |