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Título

Gold(I) complexes with alkylated PTA (1,3,5-triaza-7-phosphaadamantane) phosphanes as anticancer metallodrugs

AutorGarcía-Moreno, Elena; Gascón, Sonia; Atrián-Blasco, Elena ; Rodríguez-Yoldi, Mª. Jesus; Cerrada, Elena ; Laguna, Mariano
Palabras claveAntitumor properties
PTA
Gold
Thiolate
Water soluble
Fecha de publicación2014
EditorElsevier
CitaciónEuropean Journal of Medicinal Chemistry 79: 164-172 (2014)
ResumenNew stable thiolate gold(I) derivatives containing the alkylated phosphanes [PTA-CH2Ph]Br and [PTA-CH2COOMe]Br derived from 1,3,5-triaza-7-phosphaadamantane (PTA) have been prepared by different routes of synthesis. By the use of basic media to deprotonate the corresponding thiol in the former and by transmetallation reactions from tin (IV) complexes, in the later, thus avoiding side reactions on the phosphane. Strong antiproliferative effects are observed for most of the compounds, including the chloro- and bromo precursors with the series of phosphanes derived from PTA, in human colon cancer cell lines (Caco-2, PD7 and TC7 clones). Apoptosis-induced cell death is found for all compounds, being the thiolate derivatives with [PTA-CH2Ph]Br the most effective, as shown by an annexin-V/propidium iodide double-staining assay.©2014 Elsevier Masson SAS. All rights reserved.
URIhttp://hdl.handle.net/10261/111763
DOI10.1016/j.ejmech.2014.04.001
Identificadoresdoi: 10.1016/j.ejmech.2014.04.001
issn: 0223-5234
e-issn: 1768-3254
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