Wenzel Margot, Bigaeva Emilia, Richard Philippe, Le Gendre Pierre, Picquet Michel, Casini Angela, Bodio Ewen
Institut de Chimie Moléculaire de l'Université de Bourgogne, UMR 6302 CNRS, Université de Bourgogne, 9 avenue A. Savary, BP47870, 21078 Dijon, France.
Dept. Pharmacokinetics, Toxicology and Targeting, Groningen Research Institute of Pharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
J Inorg Biochem. 2014 Dec;141:10-16. doi: 10.1016/j.jinorgbio.2014.07.011. Epub 2014 Aug 12.
A series of mono- and heterodinuclear gold(I) and platinum(II) complexes with a new bipyridylamine-phosphine ligand have been synthesized and characterized. The X-ray structures of the ligand precursor 4-iodo-N,N-di(pyridin-2-yl)benzamide, and of one gold derivative are reported. All the complexes display antiproliferative properties in vitro in human cancer cells in the range of cisplatin or higher, which appear to correlate with compounds' uptake. Interestingly, studies of the interactions of the compounds with models of DNA indicate different mechanisms of actions with respect to cisplatin. The biological activity study of these complexes provides useful information about the interest of designing multimetallic complexes for enhanced cytotoxic properties.
合成并表征了一系列含有新型联吡啶胺 - 膦配体的单核和异双核金(I)和铂(II)配合物。报道了配体前体4 - 碘 - N,N - 二(吡啶 - 2 - 基)苯甲酰胺以及一种金衍生物的X射线结构。所有配合物在体外对人癌细胞均表现出与顺铂相当或更高的抗增殖特性,这似乎与化合物的摄取有关。有趣的是,化合物与DNA模型相互作用的研究表明其作用机制与顺铂不同。这些配合物的生物活性研究为设计具有增强细胞毒性特性的多金属配合物的研究提供了有用信息。