A review on acridinylthioureas and its derivatives: biological and cytotoxic activity

J Appl Toxicol. 2017 Oct;37(10):1132-1139. doi: 10.1002/jat.3464. Epub 2017 Mar 31.

Abstract

Acridines possess two characteristics that have led many researchers to consider the agents interesting targets for future development as potential farmacophores: the planar acridine skeleton, which is able to intercalate into DNA, and the intense fluorescence of the agents. This review offers a study of the multifunctional character of acridines and the synthesis of novel acridine derivatives, with particular focus being placed on isothiocyanates and their congeners, e.g. thioureas, isothioureas, quaternary ammonium salts and platinum/gold conjugates. The review provides an overview of the structure, spectral properties, DNA binding and biological activity of acridinylthiourea congeners. These acridinylthiourea derivatives display significant cytotoxic activities against different types of cancer cell lines at micromolar concentrations. Copyright © 2017 John Wiley & Sons, Ltd.

Keywords: Acridine; cytotoxicity; fluorescence; intercalation; isothiocyanate; platinum thioureas; synthesis; thiourea; urea.

Publication types

  • Review

MeSH terms

  • Acridines / chemical synthesis*
  • Acridines / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • DNA Damage / drug effects*
  • Humans
  • Isothiocyanates / chemical synthesis
  • Isothiocyanates / pharmacology
  • Proflavine / chemical synthesis
  • Proflavine / pharmacology
  • Structure-Activity Relationship
  • Thiourea / chemical synthesis
  • Thiourea / pharmacology

Substances

  • Acridines
  • Antineoplastic Agents
  • Isothiocyanates
  • Proflavine
  • Thiourea