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Mitochondria-targeted phosphorescent cyclometalated iridium(III) complexes: synthesis, characterization, and anticancer properties
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Mitochondria-targeted phosphorescent cyclometalated iridium(III) complexes: synthesis, characterization, and anticancer properties
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Journal Article
Mitochondria-targeted phosphorescent cyclometalated iridium(III) complexes: synthesis, characterization, and anticancer properties
2020
Overview
Cyclometalated iridium(III) complexes represent a promising approach to developing new anticancer metallodrugs. In this work, three phosphorescent cyclometalated iridium(III) complexes
Ir1–Ir3
have been explored as mitochondria-targeted anticancer agents. All three complexes display higher antiproliferative activity than cisplatin against the cancer cells screened, and with the IC
50
values ranging from 0.23 to 5.6 μM. Colocalization studies showed that these complexes are mainly localized in the mitochondria. Mechanism studies show that these complexes exert their anticancer efficacy through initiating a series of events related to mitochondrial dysfunction, including depolarization of mitochondrial membrane potential (MMP), elevation of intracellular reactive oxygen species (ROS) levels, and induction of apoptosis.
Graphic abstract
Mitochondria-targted cyclometalated iridium complexes induce apoptosis through depolarized mitochondria, elevation of intracellular ROS and activated caspase.
Publisher
Springer Berlin Heidelberg,Springer Nature B.V
Subject
/ Antineoplastic Agents - chemical synthesis
/ Antineoplastic Agents - chemistry
/ Antineoplastic Agents - pharmacology
/ Biomedical and Life Sciences
/ Cancer
/ Caspase
/ Cell Proliferation - drug effects
/ Coordination Complexes - chemical synthesis
/ Coordination Complexes - chemistry
/ Coordination Complexes - pharmacology
/ Dose-Response Relationship, Drug
/ Drug Screening Assays, Antitumor
/ Humans
/ Iridium
/ Ligands
/ Proteins
/ Reactive Oxygen Species - analysis
