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The Electron Transport Chain

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The electron transport chain or oxidative phosphorylation is an exothermic process in which free energy released during electron transfer reactions is coupled to ATP synthesis. This process is a significant source of energy in aerobic cells, and therefore inhibitors of the electron transport chain can be detrimental to the cell's metabolic processes.
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Updated: Jul 24, 2025

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor

Published on: October 26, 2017

Triarylphosphine-Coordinated Bipyridyl Ru(II) Complexes Induce Mitochondrial Dysfunction.

Richard J Mitchell¹, Anitha S Gowda¹, Alexander G Olivelli¹

¹Department of Chemistry, University of Kentucky, 505 Rose Street, Lexington, Kentucky 40506, United States.

Inorganic Chemistry

|July 5, 2023

Summary

This summary is machine-generated.

New ruthenium (Ru(II)) compounds target cancer cell mitochondria. Compound 3 selectively disrupts mitochondrial membranes, offering a promising anticancer strategy with reduced toxicity in zebrafish embryos.

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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

Area of Science:

Biochemistry
Medicinal Chemistry
Cancer Biology

Background:

Cancer cells primarily use glycolysis but rely on mitochondria for metastasis bioenergetics.
Mitochondria's role in cell death regulation makes them a key anticancer target.
Mitochondrial dysfunction is an emerging strategy for cancer therapy.

Purpose of the Study:

To synthesize and biologically characterize novel triarylphosphine-containing bipyridyl ruthenium (Ru(II)) compounds.
To investigate the impact of ligand substituents on the anticancer activity of Ru(II) compounds.
To evaluate the potential of these Ru(II) compounds as targeted anticancer agents.

Main Methods:

Synthesis of Ru(II) compounds with varying bipyridine and phosphine ligands.
Biological characterization using flow cytometry to assess mitochondrial membrane potential.
In vitro testing against cancer cells and in vivo toxicity assessment in zebrafish embryos.

Main Results:

Compound 3, with 4,4'-dimethylbipyridyl substitution, demonstrated potent mitochondrial membrane depolarization in cancer cells within minutes.
Ru(II) complex 3 induced an 8-fold increase in mitochondrial depolarization, surpassing the effect of CCCP.
Fluorinated triphenylphosphine ligands maintained anticancer potency while reducing toxicity in zebrafish embryos.

Conclusions:

Ancillary ligands significantly influence the anticancer activity of Ru(II) coordination compounds.
Ru(II) compounds capable of inducing mitochondrial dysfunction represent a promising avenue for cancer treatment.
The developed Ru(II) compounds show potential for targeted cancer therapy with an improved safety profile.