Synthesis and DNA interaction of ethylenediamine platinum(II) complexes linked to DNA intercalants
Authors
Duskova, Katerina; Sierra, Sara; Fernández, María-José; Gude Rodríguez, Lourdes; Lorente, AntonioIdentifiers
Permanent link (URI): http://hdl.handle.net/10017/20843DOI: 10.1016/j.bmc.2012.09.055
ISSN: 0968-0896
Publisher
Elsevier
Date
2012Funders
Junta de Castilla y León
Universidad de Alcalá
Ministerio de Ciencia e Innovación
Bibliographic citation
Duskova, K., Sierra, S., Fernández, M.-J, Gude, L., Lorente A. 2012. Synthesis and DNA interaction of ethylenediamine platinum(II) complexes linked to DNA intercalants. En: Bioorganic and Medicinal Chemistry, v. 20, pp. 7112-7118
Keywords
Platinum(II) complexes
DNA intercalants
DNA interactions
Project
info:eu-repo/grantAgreement/EC/FP7-PIRG05-GA-2009-248368
info:eu-repo/grantAgreement/MICINN//CTQ2011-26822/ES/SINTESIS Y EVALUACION DE LA ACTIVIDAD BIOLOGICA DE NUEVOS INHIBIDORES DE LA TELOMERASA HUMANA: LIGANDOS SELECTIVOS DEL ADN CUADRUPLE-G Y CONJUGADOS DE OLIGONUCLEOTIDOS/
info:eu-repo/grantAgreement/UAH//CCG10-UAH%2FPPQ-5961/ES/Síntesis y evaluación de la interacción biológica de nuevos inhibidores de la telomerasa
Document type
info:eu-repo/semantics/article
Version
info:eu-repo/semantics/acceptedVersion
Publisher's version
http://dx.doi.org/10.1016/j.bmc.2012.09.055Rights
Atribución-NoComercial-SinDerivadas 3.0 España
© Elsevier, 2012
Access rights
info:eu-repo/semantics/openAccess
Abstract
A series of ethylenediamine platinum(II) complexes connected through semi-rigid chains of 1,2-bis(4-
pyridyl)ethane to DNA intercalating subunits (naphthalene, anthracene or phenazine) has been synthesized,
and their interactions with calf thymus (CT) DNA have been evaluated by viscometric titrations
and equilibrium dialysis experiments. The parent ligands that contain anthracene or phenazine chromophores
showed a monointercalative mode of DNA interaction (especially the anthracene derivative),
with apparent association constants in the order of 104 M 1. The corresponding platinum(II) complexes
bind CT DNA through bisintercalation, as established by the significant increase of DNA contour length
inferred from viscosity measurements, and the association constants are in the order of 105 M 1. The
naphthalene derivatives, however, exhibit a mixed mode of interaction, which suggests a partial contribution
of both intercalation and groove binding for the ligand, and monointercalation in the case of the
platinum(II) complex. Competition dialysis experiments carried out on the intercalative compounds have
revealed a moderate selectivity towards GC DNA sequences for the derivatives containing the anthracene
chromophore.
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