Highly potent extranuclear-targeted luminescent iridium(iii) antitumor agents containing benzimidazole-based ligands with a handle for functionalization.
Jyoti YellolSergio A PérezGorakh YellolJuraj ZajacAntonio DonaireGloria ViguerasVojtech NovohradskyUlf Dietrich KahlertViktor BrabecJosé RuizPublished in: Chemical communications (Cambridge, England) (2018)
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.
Keyphrases
- quantum dots
- energy transfer
- molecular docking
- sensitive detection
- high throughput
- optical coherence tomography
- metal organic framework
- small molecule
- high resolution
- minimally invasive
- light emitting
- single molecule
- breast cancer cells
- cancer therapy
- functional connectivity
- raman spectroscopy
- high speed
- emergency department
- cell migration
- anti inflammatory
- african american
- drug delivery
- drug induced
- young adults
- label free