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Cytotoxic gold compounds: synthesis, biological characterization and investigation of their inhibition properties of the zinc finger protein PARP-1

Serratrice, Maria and Edafe, Fabio and Mendes, Filipa and Scopelliti, Rosario and Zakeeruddin, Shaik Mohammed and Grätzel, Michael and Santos, Isabel and Cinellu, Maria Agostina and Casini, Angela (2012) Cytotoxic gold compounds: synthesis, biological characterization and investigation of their inhibition properties of the zinc finger protein PARP-1. Dalton Transactions, Vol. 41 (11), p. 3287-3293. eISSN 1477-9234. Article.

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DOI: 10.1039/C2DT11913G

Abstract

The new gold(III) complexes: [Au{2-(2′-pyridyl)imidazolate}Cl2] and [Au{2,6-bis(2′-benzimidazolate)pyridine}(OCOCH3)] and the mono- and binuclear gold(I) complexes: [Au{2-(2′-pyridyl)imidazole}(PPh3)](PF6), [Au(2-phenylimidazolate)(DAPTA)] (DAPTA = 3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane), [(PPh3Au)2(2-R-imidazolate)](PF6) (R = 2-C5H4N, Ph) have been synthesized and characterized. The structure of the [(PPh3Au)2{2-(2′-pyridyl)imidazolate)](PF6) complex was also characterized by X-ray crystallography. The antiproliferative properties of the complexes were assayed against human ovarian carcinoma cell lines, either sensitive (A2780) or resistant to cisplatin (A2780cisR), human mammary carcinoma cells (MCF7) and non-tumorigenic human kidney (HEK293) cells. Most of the studied compounds showed important cytotoxic effects. Interestingly, the compounds containing the 2-(2′-pyridyl)imidazolate ligand showed selectivity towards cancer cells with respect to the non-tumorigenic ones, with the dinuclear compound [(PPh3Au)2{2-(2′-pyridyl)imidazolate)](PF6) being the most active. Some compounds were also screened for their inhibitory effect of the zinc-finger protein PARP-1, essential for DNA repair and relevant to the mechanisms of cancer cell resistance to cisplatin. Interaction studies of the compounds with the model protein ubiquitin were undertaken by electrospray ionization mass spectrometry (ESI MS). The results are discussed in relation to the putative mechanisms of action of the cytotoxic gold compounds.

Item Type:Article
ID Code:7326
Status:Published
Refereed:Yes
Uncontrolled Keywords:Cytotoxicity, PARP-1, gold compounds
Subjects:Area 03 - Scienze chimiche > CHIM/03 Chimica generale e inorganica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Royal Society of Chemistry
eISSN:1477-9234
Deposited On:04 Apr 2012 12:58

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