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To tackle this goal, the Pt<jats:sup>II<\/jats:sup> and Pt<jats:sup>IV<\/jats:sup> precursors were activated at their carboxylic acid functional group, and futher treated with the cRGDfK peptide, to afford the bioconjugates Pt<jats:sup>II<\/jats:sup>\u2013cRGD and Pt<jats:sup>IV<\/jats:sup>\u2013cRGD, respectively. Pt<jats:sup>II<\/jats:sup>\u2013cRGD was studied by <jats:sup>195<\/jats:sup>Pt NMR spectroscopy, which confirmed the presence of the Pt<jats:sup>II<\/jats:sup> center. In contrast, the characterization of Pt<jats:sup>IV<\/jats:sup>\u2013cRGD was not possible, due to the tendency of this complex to undergo reduction to Pt<jats:sup>II<\/jats:sup> in solution. Thus, only the Pt<jats:sup>II<\/jats:sup>\u2013cRGD complex was used for further biological studies, and it exhibited some cytotoxic activity against the HUVEC (human umbilical vein endothelial cells) cell line, which has the highest levels of \u03b1<jats:sub>v<\/jats:sub>\u03b2<jats:sub>3<\/jats:sub> expression. However, no improved effects were observed with respect to the Pt<jats:sup>II<\/jats:sup>\u2013pic precursor. Studies by ICP\u2010MS showed enhanced intracellular accumulation for Pt<jats:sup>II<\/jats:sup>\u2013cRGD, with respect to Pt<jats:sup>II<\/jats:sup>\u2013pic in cancer cells. Overall, these results show that, while Pt<jats:sup>II<\/jats:sup> bioconjugation enhances the uptake of the compound, it did not translate into increased cytotoxicity.<\/jats:p>","DOI":"10.1002\/ejic.201700072","type":"journal-article","created":{"date-parts":[[2017,2,10]],"date-time":"2017-02-10T05:26:40Z","timestamp":1486704400000},"page":"1835-1840","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Nonconventional <i>trans<\/i>\u2010Platinum Complexes Functionalized with RDG Peptides: Chemical and Cytototoxicity Studies"],"prefix":"10.1002","volume":"2017","author":[{"given":"Maria Angeles","family":"Medrano","sequence":"first","affiliation":[{"name":"IadChem. and Departamento de Qu\u00edmica Inorg\u00e1nica Universidad Autonoma de Madrid  28049 Madrid Spain"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7718-1629","authenticated-orcid":false,"given":"Maur\u00edcio","family":"Morais","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares Instituto Superior T\u00e9cnico Universidade de Lisboa  Estrada Nacional 10 (km 139,7) 2695\u2010066 Bobadela LRS Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5644-3199","authenticated-orcid":false,"given":"Vera F. 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