http://www.cnr.it/ontology/cnr/individuo/prodotto/ID19614

Sterically hindered complexes of platinum(II) with planar heterocyclic nitrogen donors. A novel complex with 1-methyl-cytosine has spectrum of activity different from cisplatin and is able of overcoming acquired cisplatin resistance (Articolo in rivista)

Type

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

Label

Sterically hindered complexes of platinum(II) with planar heterocyclic nitrogen donors. A novel complex with 1-methyl-cytosine has spectrum of activity different from cisplatin and is able of overcoming acquired cisplatin resistance (Articolo in rivista) (literal)

Anno

2006-01-01T00:00:00+01:00 (literal)

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

10.1016/j.jinorgbio.2006.07.010 (literal)

Alternative label

Margiotta N. 1, Natile G. 1, Capitelli F. 2, Fanizzi F.P. 3, Boccarelli A. 4, De Rinaldis P. 4, Giordano D. 4, Coluccia M. 4 (2006)
Sterically hindered complexes of platinum(II) with planar heterocyclic nitrogen donors. A novel complex with 1-methyl-cytosine has spectrum of activity different from cisplatin and is able of overcoming acquired cisplatin resistance
in Journal of inorganic biochemistry; Elsevier Science Inc., New York (Stati Uniti d'America)
(literal)

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

Margiotta N. 1, Natile G. 1, Capitelli F. 2, Fanizzi F.P. 3, Boccarelli A. 4, De Rinaldis P. 4, Giordano D. 4, Coluccia M. 4 (literal)

Pagina inizio

1849 (literal)

Pagina fine

1857 (literal)

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

100 (literal)

Rivista

Journal of inorganic biochemistry (Rivista)

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

8 (literal)

Note

ISI Web of Science (WOS) (literal)

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

1 - Dip. Farmaco-Chimico, Univ. di Bari 2 - CNR-IC, Bari 3 - Di.S.Te.B.A., Univ. di Lecce 4 - Dip. di Scienze Biomediche ed Oncologia Umana, Univ. di Bari (literal)

Titolo

Sterically hindered complexes of platinum(II) with planar heterocyclic nitrogen donors. A novel complex with 1-methyl-cytosine has spectrum of activity different from cisplatin and is able of overcoming acquired cisplatin resistance (literal)

Abstract

A very interesting series of water soluble platinum compounds violating some of the classical structure-activity relationships, but still showing antitumor activity, was reported by Hollis and collaborators some 25 years ago [L.S. Hollis, A.R. Amundsenm, E.W. Stern. J. Med. Chem. 32 (1989) 128-136]. The compounds, having formula [PtClA(2)L](+) (A(2) = two monodentate or a bidentate amine, L = a secondary or tertiary amine or a N-donor heterocycle), were characterized by a positive charge and three non-labile N-donor ligands. We have extended the investigation to analogous compounds in which 2,9-dimethyl-1,10-phenanthroline has taken the place of the A(2) ligand(s) and L is 2-picoline (1), 6-amino-2-picoline (2), or 1-methyl-cytosine (3). The X-ray analysis of 2 has revealed a bow-like distortion of the phenanthroline plane, a sloping of the phenanthroline plane with respect to the coordination plane, and an overall shielding of the metallic core by the ortho substituents of the phenanthroline and pyridine ligands. In vitro grow inhibition assays have been performed on the most water soluble complex 3. The results indicate that this complex is characterized by a potent growth inhibitory activity with mean IC50 value (in a panel of 11 human tumor cell lines) of 1.1 mu M to be compared with a mean value of 3.8 mu M for cisplatin. The same compound also appears to completely overcome the acquired cisplatin resistance stemming from reduced uptake or a multifocal mechanism, thus pointing to a mechanism of action distinctly different from that of cisplatin. (literal)

Editore