Examinando por Autor "Cabrera, Silvia"

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Enhanced Cytotoxicity and Reactivity of a Novel Platinum(IV) Family with DNA-Targeting Naphthalimide Ligands
(American Chemical Society, 2017-05-10) Navas, Francisco; Mendes, Filipa; Santos, Isabel; Navarro-Ranninger, Carmen; Cabrera, Silvia; Gómez Quiroga, Adoración
Pt(IV) complexes are known as prodrugs that can potentially overcome cisplatin limitations by slowing down its reactivity, and once reduced, act as the corresponding Pt(II) drugs. We report a new approach towards trans Pt(IV) complexes, conceived to afford nonconventional active trans Pt(II) complexes with dual targeting properties. The reduction of the complexes has been studied in the presence of ascorbic acid and glutathione, showing that different species are formed in the process. The interaction with DNA after reduction has been also studied and correlated to the formation of Pt(II) species. The cytotoxicity profile of the Pt(IV) complexes corroborated the rationale behind this approach.
Versatile Route to trans-Platinum(II) Complexes via Manipulation of a Coordinated 3‑(Pyridin-3-yl)propanoic Acid Ligand
(American Chemical Society, 2019-04-12) Cabrera, Silvia; Navas, Francisco; Matesanz, Ana I.; Maroto, Marta; Riedel, Tina; Dyson, Paul J.; Gómez Quiroga, Adoración
We describe the direct coupling of alcohols and amines to a 3-(pyridin-3-yl)propanoic acid ligand coordinated to a Pt(II) to afford ester and amide derivatives. Using this approach, a family of trans-Pt(II) compounds with amine ligands bearing long perfluorinated chains was prepared, as these chains potentially endow the complexes with thermoactivatable properties. Related compounds with alkyl chains in place of the perfluorinated chains were also prepared as controls using the same direct coupling method. The stability of the complexes in solution, their reactivity with DNA and proteins, and their antiproliferative activity evaluated in tumorigenic (A2780 and A2780cisR) and nontumorigenic (HEK293) cells at 37 °C and following exposure to elevated temperatures (that mimic the temperatures employed in thermotherapy) were also studied to assess their utility as putative (thermoactivated) anticancer agents.