Derivatization of Preformed Platinum N-Heterocyclic Carbene Complexes with Amino Acid and Peptide Ligands and Cytotoxic Activities toward Human Cancer Cells.

Fiche publication


Date publication

novembre 2012

Auteurs

Membres identifiés du Cancéropôle Est :
Dr BELLEMIN-LAPONNAZ Stéphane


Tous les auteurs :
Chardon E, Dahm G, Guichard G, Bellemin-Laponnaz S

Résumé

A simple procedure for the preparation of N-heterocyclic carbene platinum complexes with a nitrogen-based neutral ligand in trans geometry is presented. The lability of a trans pyridine ligand in an N-heterocyclic carbene-Pt(II)-pyridine complex, namely, (3-benzyl-1-methylimidazolylidene)PtI2-pyridine), 2, was probed by a displacement reaction with various nitrogen-based ligands (e.g., amines, hydrazine, amino esters, and peptides) to yield the corresponding complexes, which could be easily isolated by column chromatography. Two representative complexes could be characterized by X-ray crystallographic studies. This strategy allows generating diversity in metallodrug candidates. Preliminary results of the biological effects on various human cancer cells and comparison wih cisplatin are reported.

Référence

Organometallics. 2012 Nov 12;31(21):7618-21.