| Literature DB >> 31441186 |
Dalila Rocco1, Lucinda K Batchelor2, Gabriele Agonigi1, Simona Braccini1, Federica Chiellini1, Silvia Schoch1, Tarita Biver3, Tiziana Funaioli1, Stefano Zacchini4, Lorenzo Biancalana1, Marina Ruggeri1, Guido Pampaloni1, Paul J Dyson2, Fabio Marchetti1.
Abstract
Although ferrocene derivatives have attracted considerable attention as possible anticancer agents, the medicinal potential of diiron complexes has remained largely unexplored. Herein, we describe the straightforward multigram-scale synthesis and the antiproliferative activity of a series of diiron cyclopentadienyl complexes containing bridging vinyliminium ligands. IC50 values in the low-to-mid micromolar range were determined against cisplatin sensitive and resistant human ovarian carcinoma (A2780 and A2780cisR) cell lines. Notable selectivity towards the cancerous cells lines compared to the non-tumoral human embryonic kidney (HEK-293) cell line was observed for selected compounds. The activity seems to be multimodal, involving reactive oxygen species (ROS) generation and, in some cases, a fragmentation process to afford monoiron derivatives. The large structural variability, amphiphilic character and good stability in aqueous media of the diiron vinyliminium complexes provide favorable properties compared to other widely studied classes of iron-based anticancer candidates.Entities:
Keywords: complexes; cytotoxicity; iron; metal-based drugs; vinyliminium ligands
Year: 2019 PMID: 31441186 DOI: 10.1002/chem.201902885
Source DB: PubMed Journal: Chemistry ISSN: 0947-6539 Impact factor: 5.236