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- Title
A Chemical-Biological Evaluation of Rhodium(I) N-Heterocyclic Carbene Complexes as Prospective Anticancer Drugs.
- Authors
Oehninger, Luciano; Küster, Laura Nadine; Schmidt, Claudia; Muñoz‐Castro, Alvaro; Prokop, Aram; Ott, Ingo
- Abstract
Rhodium(I) complexes bearing N-heterocyclic carbene (NHC) ligands have been widely used in catalytic chemistry, but there are very few reports of biological properties of these organometallics. A series of RhI-NHC derivatives with 1,5-cyclooctadiene and CO as secondary ligands were synthesized, characterized, and biologically investigated as prospective antitumor drug candidates. Pronounced antiproliferative effects were noted for all complexes, along with moderate inhibitory activity of thioredoxin reductase (TrxR) and efficient binding to biomolecules (DNA, albumin). Biodistribution studies showed that the presence of albumin lowered the cellular uptake and confirmed the transport of rhodium into the nuclei. Changes in the mitochondrial membrane potential (MMP) were observed as well as DNA fragmentation in wild-type and daunorubicin- or vincristine-resistant Nalm-6 leukemia cells. Overall, these studies indicated that RhI-NHC fragments could be used as partial structures of new antitumor agents, in particular in those drugs designed to address resistant malignant tissues.
- Subjects
HETEROCYCLIC chemistry; RHODIUM; ANTINEOPLASTIC agents; HETEROCYCLIC compounds; DNA; THIOREDOXIN
- Publication
Chemistry - A European Journal, 2013, Vol 19, Issue 52, p17871
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201302819