Muenzner, Julienne K, Biersack, Bernhard, Albrecht, Alexander, Rehm, Tobias, Lacher, Ulrike, Milius, Wolfgang, Casini, Angela  ORCID: https://orcid.org/0000-0003-1599-9542, 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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Abstract
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: | 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: | 06 Nov 2024 05:30 |
| URI: | https://orca.cardiff.ac.uk/id/eprint/95519 |
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