Recent advances in α,β-unsaturated carbonyl compounds as mitochondrial toxins

Eur J Med Chem. 2019 Dec 1:183:111687. doi: 10.1016/j.ejmech.2019.111687. Epub 2019 Sep 9.

Abstract

Conjugated α,β-unsaturated ketones are very useful compounds associated with diverse medicinal properties. This review outlines α,β-unsaturated ketones as candidate cytotoxic agents which affect mitochondrial function. Both naturally occurring compounds and synthetic chemicals have been discussed which exert their cytotoxic effects, at least in part, by acting on mitochondria. Biochemical differences between tumour mitochondria and this organelle in non-malignant cells have been exploited to investigate various compounds that can cause greater toxicity to neoplasms than normal cells. On a number of instances, correlations between the structures of various α,β-unsaturated ketones and cytotoxic potencies have been observed. The aspiration is that this review will assist drug designers to create compounds which are significantly more toxic to neoplasms than normal tissues.

Keywords: Chalcones; Curcumin; Cytotoxins; Mitochondria; Structure-activity relationships; Tumors; α,β-unsaturated ketones.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Ketones / chemistry
  • Ketones / pharmacology*
  • Mitochondria / drug effects*
  • Mitochondria / metabolism
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism

Substances

  • Ketones