Premium
DNA Binding Studies and Cytotoxicity of a Dinuclear Pt II Diazapyrenium‐Based Metallo‐supramolecular Rectangular Box
Author(s) -
Terenzi Alessio,
Ducani Cosimo,
Blanco Víctor,
Zerzankova Lenka,
Westendorf Aron F.,
Peinador Carlos,
Quintela José M.,
Bednarski Patrick J.,
Barone Giampaolo,
Han Michael J.
Publication year - 2012
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201201519
Subject(s) - metallacycle , circular dichroism , intercalation (chemistry) , binding constant , supramolecular chemistry , ligand (biochemistry) , dna , stereochemistry , crystallography , chemistry , binding site , physics , biochemistry , crystal structure , x ray crystallography , inorganic chemistry , receptor , diffraction , optics
The interaction with native DNA of a 2,7‐diazapyrenium‐based ligand 1 and its Pt II rectangular metallacycle 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 binding 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 IC 50 values ranging between 3.1 and 19.2 μ M and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin.