A series of imidazole based platinum(II) complexes were synthesised and evaluated for their cytotoxicity in HCT-116 cancer cell line, known for being partially resistant to cisplatin but sensitive to oxaliplatin. Lipophilicity was modulated by introducing differently long saturated and unsaturated chains at the N1 of the imidazole moiety. Pt-I displayed the higher cytotoxic effect achieving a IC50 = 38.0 ± 14.1 μM, comparable to the oxaliplatin value. The interaction between the imidazole platinum(II) complexes and the octapeptide called Mets7, the methionine-rich motif mimicking the N-terminal domain of the yCtr-1, was evaluated in order to have a major insight of the uptake and the eventual resistance mechanisms for the so-synthesised novel platinum compounds.
Promising antiproliferative platinum(II) complexes based on imidazole moiety: synthesis, evaluation in HCT-116 cancer cell line and interaction with Ctr-1 Met-rich domain / N. Ferri, G. Facchetti, S. Pellegrino, C. Ricci, G. Curigliano, E. Pini, I. Rimoldi. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 1464-3391. - 23:10(2015 May 15), pp. 2538-2547.
|Titolo:||Promising antiproliferative platinum(II) complexes based on imidazole moiety: synthesis, evaluation in HCT-116 cancer cell line and interaction with Ctr-1 Met-rich domain|
|Parole Chiave:||Imidzazole; Platinum(II) complex; Antiproliferative compound; HCT-116; Mets7|
|Settore Scientifico Disciplinare:||Settore CHIM/03 - Chimica Generale e Inorganica|
Settore BIO/14 - Farmacologia
Settore CHIM/06 - Chimica Organica
|Data di pubblicazione:||15-mag-2015|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.bmc.2015.03.044|
|Appare nelle tipologie:||01 - Articolo su periodico|