Small-Molecule Inhibitors of Reactive Oxygen Species Production

Elisa Sassetti, Mads Hartvig Clausen*, Luca Laraia*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review


Reactive oxygen species (ROS) are involved in physiological cellular processes including differentiation, proliferation, and apoptosis by acting as signaling molecules or regulators of transcription factors. The maintenance of appropriate cellular ROS levels is termed redox homeostasis, a balance between their production and neutralization. High concentrations of ROS may contribute to severe pathological events including cancer, neurodegenerative, and cardiovascular diseases. In recent years, approaches to target the sources of ROS production directly in order to develop tool compounds or potential therapeutics have been explored. Herein, we briefly outline the major sources of cellular ROS production and comprehensively review the targeting of these by small-molecule inhibitors. We critically assess the value of ROS inhibitors with different mechanisms-of-action, including their potency, mode-of-action, known off-target effects, and clinical or preclinical status, while suggesting future avenues of research in the field.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Issue number9
Pages (from-to)5252-5275
Number of pages24
Publication statusPublished - 2021


  • Oxides
  • Inhibitors
  • Peptides and proteins
  • Free radical
  • Antioxidants


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