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Binding studies of metal–salphen and metal–bipyridine complexes towards G‐Quadruplex DNA Łęczkowska, Anna . González García, Jorge . Pérez Arnáiz, Cristina García Ruiz, Begoña White, Andrew J. P. . Vilar, Ramón . cancer DNA binding heterocycles metal complexes polymerase Química física Chemistry, Physical and theoretical The proposed in vivo formation of G-quadruplex DNA (G4 DNA) in promoter regions of oncogenes and in telomeres has prompted the development of small molecules with high affinity and selectivity for these structures. Herein we report the synthesis of a new di-substituted bipyridine ligand and the corresponding complexes with Ni2+ and VO2+. Both these new complexes have been characterized spectroscopically and by X-ray crystallography. Detailed DNA binding studies of these two complexes, together with three previously reported metal salphen complexes, are presented. Using FRET melting assays, the binding affinity and selectivity of the five metal complexes against six different G4 DNA structures as well as a duplex DNA have been determined. In addition, we present detailed ITC and UV/Vis studies to characterize the interaction of the complexes with human telomeric G4 DNA. Finally, we show via a polymerase stop assay that these complexes are able to stabilize a G4 DNA structure (from the c-Myc oncogene promoter) and halt the activity of Taq polymerase. UK’s Engineering and Physical Sciences Research Council (EPSRC) (grant number: EP/H005285/1) 2018-09-05T09:24:03Z 2019-08-09T02:45:06Z 2018-08 info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion 0947-6539 http://hdl.handle.net/10259/4911 10.1002/chem.201802248 eng Chemistry-a european journal. 2018, V. 24, n. 45, p. 11785-11794 https://doi.org/10.1002/chem.201802248 info:eu-repo/grantAgreement/EPSRC/EP/H005285/1 info:eu-repo/semantics/openAccess application/pdf Wiley-VCH Verlag