Benzyl-substituted metallocarbene antibiotics and anticancer drugs.
Benzyl-substituted metallocarbene compounds synthesised by our group and others during the past 5 years give a new perspective on their activity as antibiotic and antitumoral drugs. N-heterocyclic carbenes containing an imidazole core were functionalised and their transition metal complexes (M = Ag, Au, Cu, Ru) have shown promising antibacterial as well as anticancer activity in vitro and in vivo. IC50 values in the nanomolar region or antibacterial activity comparable to conventional antibiotics lead the way towards novel drug candidates.
University College Dublin, Belfield, Dublin 4, Ireland. fraukehackenberg@web.de matthias.tacke@ucd.ie.
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D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001593:Benzyl Compounds / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003300:Copper / Q000737:chemistry; D006046:Gold / Q000737:chemistry; D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D019216:Metals, Heavy / Q000737:chemistry*; D008697:Methane / Q000031:analogs & derivatives* / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D012428:Ruthenium / Q000737:chemistry; D012834:Silver / Q000737:chemistry
D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D001593:Benzyl Compounds; D007093:Imidazoles; D019216:Metals, Heavy; C030011:carbene; D012834:Silver; D006046:Gold; D003300:Copper; D012428:Ruthenium; D008697:Methane