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Ferrocenyl-coupled n-heterocyclic carbene complexes of gold(i): a successful approach to multinuclear anticancer drugs

Muenzner, Julienne K, Biersack, Bernhard, Albrecht, Alexander, Rehm, Tobias, Lacher, Ulrike, Milius, Wolfgang, Casini, Angela ORCID:, Zhang, Jing-Jing, Ott, Ingo, Brabec, Viktor, Stuchlikova, Olga, Andronache, Ion C, Schuppan, Detlef, Kaps, Leonard and Schobert, Rainer 2016. Ferrocenyl-coupled n-heterocyclic carbene complexes of gold(i): a successful approach to multinuclear anticancer drugs. Chemistry - a European Journal 22 (52) , pp. 18953-18962. 10.1002/chem.201604246

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Four gold(I) carbene complexes featuring 4-ferrocenyl substituted imidazol-2-ylidene ligands were investigated for antiproliferative and antivascular properties. They were active against a panel of seven cancer cell lines, including multidrug-resistant ones, with low micromolar or nanomolar IC50 (72 h) values, according to their lipophilicity and cellular uptake. The delocalised lipophilic cationic complexes 8 and 10 acted by increasing the reactive oxygen species in two ways: via a genuine ferrocene effect and by inhibiting the thioredoxin reductase. Both complexes gave rise to a reorganization of the F-actin cytoskeleton in endothelial and melanoma cells, associated with a G1 phase cell cycle arrest and a retarded cell migration. They proved antiangiogenic in tube formation assays with endothelial cells and vascular-disruptive on real blood vessels in the chorioallantoic membrane of chicken eggs. Biscarbene complex 10 was also tolerated well by mice where it led to a volume reduction of xenograft tumors by up to 80%.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Uncontrolled Keywords: antitumor agents; carbenes; metal-based drugs; gold; antivascular activity
Publisher: WileyBlackwell
ISSN: 0947-6539
Date of First Compliant Deposit: 21 October 2016
Date of Acceptance: 19 October 2016
Last Modified: 28 Nov 2022 16:08

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