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.
Accelerating Research
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom
Address
John Eccles HouseRobert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom