http://www.cnr.it/ontology/cnr/individuo/prodotto/ID18477

Synthesis, in vitro and in vivo characterization of 64Cu(I) complexes derived from hydrophilic tris(hydroxymethyl)phosphane and 1,3,5-triaza-7-phosphaadamantane ligands (Articolo in rivista)

Type

Prodotto della ricerca (Classe)
Articolo in rivista (Classe)

Label

Synthesis, in vitro and in vivo characterization of 64Cu(I) complexes derived from hydrophilic tris(hydroxymethyl)phosphane and 1,3,5-triaza-7-phosphaadamantane ligands (Articolo in rivista) (literal)

Anno

2008-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

10.1007/s00775-007-0322-y (literal)

Alternative label

Alidori S.; Gioia Lobbia G.; Papini G.; Pellei M.; Porchia M.; Refosco F.; Tisato F.; Lewis J. S.; Santini C. (2008)
Synthesis, in vitro and in vivo characterization of 64Cu(I) complexes derived from hydrophilic tris(hydroxymethyl)phosphane and 1,3,5-triaza-7-phosphaadamantane ligands
in JBIC. Journal of biological inorganic chemistry (Print); Springer, New York (Stati Uniti d'America)
(literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

Alidori S.; Gioia Lobbia G.; Papini G.; Pellei M.; Porchia M.; Refosco F.; Tisato F.; Lewis J. S.; Santini C. (literal)

Pagina inizio

307 (literal)

Pagina fine

315 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#url

http://www.springerlink.com/content/u602n60761210360/fulltext.pdf (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

13 (literal)

Rivista

JBIC. Journal of biological inorganic chemistry (Rivista)

Note

Scopu (literal)
ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

1-4,9 : Dipartimento di Scienze Chimiche, Università di Camerino / 5-7 : ICIS-CNR, Padova / 8: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis (literal)

Titolo

Synthesis, in vitro and in vivo characterization of 64Cu(I) complexes derived from hydrophilic tris(hydroxymethyl)phosphane and 1,3,5-triaza-7-phosphaadamantane ligands (literal)

Abstract

Four novel Cu-64 complexes ([Cu-64(thp)(4)](+) (1), [Cu-64(TPA)(4)](+) (2), [HC(CO2)(pz(Me2))(2) Cu-64(thp)(2)] (3) and [HC(CO2)(tz)(2) 64Cu(thp)(2)] (4), [where thp is tris(hydroxymethyl)phosphine, TPA is 1,3,5-triaza-7-phosphaadamantane, pz(Me2) is 3,5-dimethylpyrazole and tz is 1,2,4-triazole] were successfully synthesized and characterized. The complexes were produced in high radiochemical purity and yield (more than 98%) without the need for further purification. Their logP values and serum stabilities were measured and in vitro behavior was observed in cultured EMT-6 cells. The logP values (+/- standard deviation) obtained were -2.26 +/- 0.04 (1), 0.01 +/- 0.01 (2), -1.24 +/- 0.03 (3) and -2.06 +/- 0.03 (4). Complex 3 demonstrated the highest serum stability, with approximately 33% of the complex still intact after 1-h incubation. Complex 2 showed a rapid cell-association with EMT-6 cells, with more than 8.5% association at 2 h. This association was significantly higher (P < 0.001) than for the other three compounds after a 2-h incubation (1, 1.21%; 3, 0.63%; 4, 2.75%). Biodistribution and small-animal positron emission tomography/computed tomography was undertaken with 1 in mice bearing EMT-6 tumors. EMT-6 tumor uptake was high at 1 h (7.71 +/- 2.17 %ID/g) and decreased slowly over 24 h (4 h, 4.90 +/- 0.78 %ID/g; 24 h, 3.74 +/- 0.73 %ID/g). The PET/CT images show that the EMT-6 tumors can be visualized at all time points. In this proof-of-concept study, we have successfully synthesized and characterized a novel series of versatile water-soluble Cu(I) complexes containing monophosphine ligands. We also report the use of 1 as a building block for new radiopharmaceuticals, perhaps the first time such a method has been used in the production of copper radiopharmaceuticals. (literal)

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