Targeting cancer cell metabolism with mitochondria-immobilized phosphorescent cyclometalated iridium(iii) complexes.

ABSTRACT: Cancer cell metabolism is reprogrammed to sustain the high metabolic demands of cell proliferation. Recently, emerging studies have shown that mitochondrial metabolism is a potential target for cancer therapy. Herein, four mitochondria-targeted phosphorescent cyclometalated iridium(iii) complexes have been designed and synthesized. Complexes 2 and 4, containing reactive chloromethyl groups for mitochondrial fixation, show much higher cytotoxicity than complexes 1 and 3 without mitochondria-immobilization properties against the cancer cells screened. Further studies show that complexes 2 and 4 induce caspase-dependent apoptosis through mitochondrial damage, cellular ATP depletion, mitochondrial respiration inhibition and reactive oxygen species (ROS

SUBMITTER: Cao JJ 

PROVIDER: S-EPMC5933427 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature