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 a bridging vinyliminium ligand. IC50 values in the low to mid-micromolar range were assessed against cisplatin sensitive and resistant human ovarian carcinoma (A2780 and A2780cisR) cell lines. Notable selectivity towards the cancerous cells lines compared to the non-tumoural human embryonic kidney (HEK-293) cell line was observed for selected compounds. The mode of action is attributed to a one electron reduction process, which results in a fragmentation releasing an activated mononuclear iron derivative. The large structural variability, amphiphilic character and good stability in aqueous media of the diiron vinyliminium complexes collectively provide favourable properties compared to other widely studied classes of iron-based anticancer candidates. .
Rocco D., Batchelor L.K., Agonigi G., Braccini S., Chiellini F., Schoch S., et al. (2019). Anticancer Potential of Diiron Vinyliminium Complexes. CHEMISTRY-A EUROPEAN JOURNAL, 25(65), 14801-14816 [10.1002/chem.201904317].
Anticancer Potential of Diiron Vinyliminium Complexes
Zacchini S.;
2019
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 a bridging vinyliminium ligand. IC50 values in the low to mid-micromolar range were assessed against cisplatin sensitive and resistant human ovarian carcinoma (A2780 and A2780cisR) cell lines. Notable selectivity towards the cancerous cells lines compared to the non-tumoural human embryonic kidney (HEK-293) cell line was observed for selected compounds. The mode of action is attributed to a one electron reduction process, which results in a fragmentation releasing an activated mononuclear iron derivative. The large structural variability, amphiphilic character and good stability in aqueous media of the diiron vinyliminium complexes collectively provide favourable properties compared to other widely studied classes of iron-based anticancer candidates. .I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
