Enhanced Anticancer Selectivity of Cyclometalated Imidazole/Pyrazole-Imine Iridium Complexes Through the Switch from Cationic to Zwitterionic Forms.

Cyclometalated iridium complexes have shown promising anticancer properties, with variations in charge and ligand substitution significantly influencing their biological activity. However, zwitterionic iridium complexes remain scarcely explored. Herein, we report a series of zwitterionic cyclometalated imidazole/pyrazole-imine iridium complexes and compare their biological activity to analogous cationic complexes with sulfonate counteranions.

Triphenylphosphine-modified cyclometalated iridium complexes as mitochondria-targeting anticancer agents with enhanced selectivity.

This study presents the development and evaluation of triphenylphosphine-modified cyclometalated iridium complexes as selective anticancer agents targeting mitochondria. By leveraging the mitochondrial localization capability of the triphenylphosphine group, these complexes displayed promising cytotoxicity in the micromolar range (3.12-7.

Triphenylphosphine-Modified Iridium, Rhodium, and Ruthenium Complexes to Achieve Enhanced Anticancer Selectivity by Targeting Mitochondria.

The incorporation of an organelle-targeting moiety into compounds has proven to be an effective strategy in the development of targeted anticancer drugs. We herein report the synthesis, characterization, and biological evaluation of novel triphenylphosphine-modified half-sandwich iridium, rhodium, and ruthenium complexes. The primary goal was to enhance anticancer selectivity through mitochondrial targeting.

Iminoamido chelated iridium(III) and ruthenium(II) anticancer complexes with mitochondria-targeting ability and potential to overcome cisplatin resistance.

A diverse set of neutral half-sandwich iminoamido iridium and ruthenium organometallic complexes is synthesized through the utilization of Schiff base pro-ligands with NN donors. Notably, these metal complexes with varying leaving groups (Cl or OAc) are formed by employing different quantities of the deprotonating agent NaOAc, and exhibit promising cytotoxicity against various cancer cell lines such as A549 and cisplatin-resistant A549/DDP lung cancer cells, as well as HeLa cells, with IC values spanning from 9.26 to 15.

Mitochondria-targeted neutral and cationic iridium(III) anticancer complexes chelating simple hybrid sp-N/sp-N donor ligands.

Most platinum group-based cyclometalated neutral and cationic anticancer complexes with the general formula [(C^N)Ir(XY)] (neutral complex: XY = bidentate anionic ligand; cationic complex: XY = bidentate neutral ligand) are notable owing to their intrinsic luminescence properties, good cell permeability, interaction with some biomolecular targets and unique mechanisms of action (MoAs). We herein synthesized a series of neutral and cationic amine-imine cyclometalated iridium(III) complexes using Schiff base ligands with sp-N/sp-N N^NH chelating donors. The cyclometalated iridium(III) complexes were identified by various techniques.