Acridine as an Anti-Tumour Agent: A Critical Review

Molecules. 2022 Dec 26;28(1):193. doi: 10.3390/molecules28010193.

Abstract

This review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines are well-known for their high cytotoxic activity; however, their clinical application is restricted or even excluded as a result of side effects. The photocytotoxicity of propyl acridine acts against leukaemia cell lines, with C1748 being a promising anti-tumour drug against UDP-UGT's. CK0403 is reported in breast cancer treatment and is more potent than CK0402 against estrogen receptor-negative HER2. Acridine platinum (Pt) complexes have shown specificity on the evaluated DNA sequences; 9-anilinoacridine core, which intercalates DNA, and a methyl triazene DNA-methylating moiety were also studied. Acridine thiourea gold and acridinone derivatives act against cell lines such as MDA-MB-231, SK-BR-3, and MCF-7. Benzimidazole acridine compounds demonstrated cytotoxic activity against Dual Topo and PARP-1. Quinacrine, thiazacridine, and azacridine are reported as anti-cancer agents, which have been reported in the previous decade and were addressed in this review article.

Keywords: DNA-intercalation; acridine; anti-cancer; cancer cell lines; in vitro assay; topoisomerase.

Publication types

  • Review

MeSH terms

  • Acridines / chemistry
  • Acridines / pharmacology
  • Antineoplastic Agents* / chemistry
  • Breast Neoplasms* / drug therapy
  • Cell Line
  • Cell Line, Tumor
  • DNA / metabolism
  • Female
  • Humans
  • Intercalating Agents / pharmacology

Substances

  • Antineoplastic Agents
  • Intercalating Agents
  • DNA
  • Acridines

Grants and funding

This research received no external funding.