Rational design of gold(III)-dithiocarbamato peptidomimetics for the targeted anticancer chemtherapy (Articolo in rivista)

Type
Label
  • Rational design of gold(III)-dithiocarbamato peptidomimetics for the targeted anticancer chemtherapy (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.jinorgbio.2012.07.001 (literal)
Alternative label
  • M. Negom Kouodom; G. Boscutti; M. Celegato; M. Crisma; S. Sitran; D. Aldinucci; F. Formaggio; L. Ronconi; D. Fregona (2012)
    Rational design of gold(III)-dithiocarbamato peptidomimetics for the targeted anticancer chemtherapy
    in Journal of inorganic biochemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • M. Negom Kouodom; G. Boscutti; M. Celegato; M. Crisma; S. Sitran; D. Aldinucci; F. Formaggio; L. Ronconi; D. Fregona (literal)
Pagina inizio
  • 248 (literal)
Pagina fine
  • 260 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 117 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • a Department of Chemical Sciences, University of Padova, Via F. Marzolo 1, Padova 35131, Italy b Division of Experimental Oncology 2, Centro di Riferimento Oncologico (CRO-IRCSS), Via F. Gallini 2, Aviano (PN) 33081, Italy c Institute of Biomolecular Chemistry, CNR, Padova Unit, Via F. Marzolo 1, Padova 35131, Italy d Institute of Inorganic and Surfaces Chemistry, CNR Research Area, Corso Stati Uniti 4, Padova 35127, Italy (literal)
Titolo
  • Rational design of gold(III)-dithiocarbamato peptidomimetics for the targeted anticancer chemtherapy (literal)
Abstract
  • As a further extension of our researchwork focusing on the development of gold(III)-dithiocarbamato dtc derivatives of oligopeptides as potential anticancer agents, complexes [AuIIIX2(dtc-Sar-L-Ser(t-Bu)-O(t-Bu))] (X=Br (1a)/Cl (1b)), [AuIIIX2(dtc-AA-Aib2-O(t-Bu))] (AA=Sar (sarcosine, N-methylglycine), X=Br (2a)/Cl (2b); AA=D,L-Pro, X=Br (3a)/Cl (3b)), [AuIIIX2(dtc-Sar-Aib3-O(t-Bu))] (X=Br (4a)/Cl (4b)), and [AuIIIX2(- dtc-Sar-Aib3-Gly-OEt)] (X=Br (5a)/Cl (5b)) (Aib = \"alpha\"-aminoisobutyric acid, 2-methylalanine) were designed to obtain metal-based peptidomimetics that may specifically target two peptide transporters (namely, PEPT1 and PEPT2) upregulated in several human tumor cells. All the compoundswere characterized by means of FT-IR and mono- and multidimensional NMR spectroscopy. According to in vitro cytotoxicity studies, complex [AuIIICl2(dtc-D,L-Pro-Aib2-O(t-Bu))] (3b) turned out to be the most effective toward the four human tumor cell lines evaluated (PC3, 2008, C13, and L540), for which the IC50 values were lower than cisplatin. Remarkably, it showed no cross-resistance with cisplatin itself and was proved to inhibit tumor cell proliferation by inducing almost exclusively late apoptosis/necrosis. Biological results are here reported and discussed in terms of the structure-activity relationship. (literal)
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