Publication
Tricarbonyl M(I) (M = Re, 99mTc) complexes bearing acridine fluorophores : synthesis, characterization, DNA interaction studies and nuclear targeting
| dc.contributor.author | Esteves, Teresa | |
| dc.contributor.author | Xavier, Catarina | |
| dc.contributor.author | Gama, Sofia | |
| dc.contributor.author | Mendes, Filipa | |
| dc.contributor.author | Raposinho, Paula D. | |
| dc.contributor.author | Marques, Fernanda | |
| dc.contributor.author | Paulo, António | |
| dc.contributor.author | Pessoa, João Costa | |
| dc.contributor.author | Rino, José | |
| dc.contributor.author | Viola, Giampietro | |
| dc.contributor.author | Santos, Isabel | |
| dc.date.accessioned | 2012-10-25T14:22:04Z | |
| dc.date.available | 2012-10-25T14:22:04Z | |
| dc.date.issued | 2010 | |
| dc.description | © The Royal Society of Chemistry 2010 | por |
| dc.description.abstract | New pyrazolyl-diamine ligands with acridine derivatives at the 4-position of the pyrazolyl ring were synthesized and characterized (L1 and L2). Coordination towards the fac-[M(CO)3]+ (M = Re, 99mTc) led to complexes fac-[M(CO)3(κ3-L)] (L = L1: M = Re1, Tc1; L = L2: M = Re2, Tc2). The interaction of the novel pyrazolyl-diamine ligands (L1 and L2) and rhenium(I) complexes (Re1 and Re2) with calf thymus DNA (CT-DNA) was investigated by a variety of techniques, namely UV-visible , fluorescence spectroscopy and circular and linear dichroism . Compounds L1 and Re1 have moderate affinity to CT-DNA and bind to DNA by intercalation, while L2 and Re2 have a poor affinity for CT-DNA. Moreover, LD measurements showed that L1 and Re1 act as perfect intercalators . By confocal fluorescence microscopy we found that L1 and Re1 internalize and localize in the nucleus of B16F1 murine melanoma cells . The congener Tc1 complex also targets the cell nucleus exhibiting a time-dependent cellular uptake and a fast and high nuclear internalization (67.2% of activity after 30 min). Plasmid DNA studies have shown that Tc1 converts supercoiled (sc) puc19 DNA to the open circular (oc) form. | eng |
| dc.description.sponsorship | Teresa Esteves and Sofia Gama thank the FCT for a doctoral and postdoctoral research grants (SFRH/BD/29154/2006 and SFRH/BPD/29564/2006, respectively). COST Action D39 is also acknowledge. The QITMS instrument was acquired with the support of the Programa Nacional de Reequipamento Científico (Contract>REDE/1503/REM/2005-ITN) of Fundação para a Ciência e a Tecnologia and is part of RNEM - Rede Nacional de Espectrometria de Massa. | eng |
| dc.identifier.citation | Org. Biomol. Chem., 2010, 8, 4104-4116 | eng |
| dc.identifier.issn | 1477-0520 | |
| dc.identifier.uri | http://dx.doi.org/10.1039/C0OB00073F | |
| dc.identifier.uri | http://hdl.handle.net/10451/7119 | |
| dc.language.iso | eng | por |
| dc.peerreviewed | yes | por |
| dc.publisher | Royal Society of Chemistry | eng |
| dc.subject | Acridine | eng |
| dc.subject | Fluorescence spectroscopy | eng |
| dc.subject | Radiopharmaceuticals | eng |
| dc.subject | Cell nucleus | eng |
| dc.subject | DNA | eng |
| dc.title | Tricarbonyl M(I) (M = Re, 99mTc) complexes bearing acridine fluorophores : synthesis, characterization, DNA interaction studies and nuclear targeting | por |
| dc.type | journal article | |
| dspace.entity.type | Publication | |
| oaire.citation.endPage | 4116 | por |
| oaire.citation.startPage | 4104 | por |
| oaire.citation.title | Organic and Biomolecular Chemistry | eng |
| oaire.citation.volume | 8 | por |
| rcaap.rights | openAccess | por |
| rcaap.type | article | por |