Molecules (Dec 2022)

Acridine as an Anti-Tumour Agent: A Critical Review

  • Potlapati Varakumar,
  • Kalirajan Rajagopal,
  • Baliwada Aparna,
  • Kannan Raman,
  • Gowramma Byran,
  • Clara Mariana Gonçalves Lima,
  • Salma Rashid,
  • Mohammed H. Nafady,
  • Talha Bin Emran,
  • Sławomir Wybraniec

DOI
https://doi.org/10.3390/molecules28010193
Journal volume & issue
Vol. 28, no. 1
p. 193

Abstract

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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.

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