Highly potent extranuclear-targeted luminescent iridium(iii) antitumor agents containing benzimidazole-based ligands with a handle for functionalization
Language English Country England, Great Britain Media print
Document type Journal Article
PubMed
27869279
DOI
10.1039/c6cc07909a
Knihovny.cz E-resources
- MeSH
- Benzimidazoles chemistry pharmacology MeSH
- Iridium chemistry pharmacology MeSH
- Microscopy, Confocal MeSH
- Humans MeSH
- Ligands MeSH
- Luminescence * MeSH
- Molecular Structure MeSH
- Cell Line, Tumor MeSH
- Organometallic Compounds chemical synthesis chemistry pharmacology MeSH
- Cell Proliferation drug effects MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Drug Screening Assays, Antitumor MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- benzimidazole MeSH Browser
- Benzimidazoles MeSH
- Iridium MeSH
- Ligands MeSH
- Organometallic Compounds MeSH
- Antineoplastic Agents MeSH
A series of 6 substitutionally inert and luminescent iridium(iii) antitumor agents of the type [Ir(C∧N)2(N∧N)][PF6] containing a benzimidazole N∧N ligand with an ester group as a handle for further functionalization has been prepared. They exhibit IC50 values in the high nanomolar range in some ovarian and breast cancer cell lines (approximately 100× more cytotoxic than cisplatin (CDDP) in MDA-MB-231) and are located in the actin cortex predominantly as shown by confocal luminescence microscopy. This discovery could open the door to a new large family of drug bioconjugates with diverse and simultaneous functions.
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