An insight into recent developments in imidazole based heterocyclic compounds as anticancer agents: Synthesis, SARs, and mechanism of actions

Eur J Med Chem. 2024 Dec 15:280:116896. doi: 10.1016/j.ejmech.2024.116896. Epub 2024 Sep 21.

Abstract

Among all non-communicable diseases, cancer is ranked as the second most common cause of death and is rising constantly. While cancer treatments mainly include radiation therapy, chemotherapy, and surgery; chemotherapy is considered the most commonly employed and effective treatment. Most of the chemotherapeutic agents are azoles based compounds and imidazole is one such insightful azole. The anticancer properties of imidazole-based compounds have been thoroughly explored in recent years and all monosubstituted, disubstituted, trisubstituted, and tetrasubstituted imidazoles have been explored for their anticancer activities. Along with these compounds, other imidazole-based compounds like 1,3-dihydro-2H-imidazole-2-thiones, imidazolones, and poly imidazole compounds have also been explored for their anticancer activities. The activities of these compounds are heavily influenced by their structural resemblance to combretastatin 4A and ABI (2-aryl-4-benzoyl-imidazole). The lead compounds were highly active on breast, gastric, colon, ovarian, cervical, bone marrow, melanoma, prostate, lung, leukemic, neuroblastoma, liver, Ehrlich, melanoma, and pancreatic cancers. The targets of these leads like tubulin, heme oxygenases, VEGF, tyrosine kinases, EGFR, and others have also been explored. The exploration of the anticancer potential of substituted imidazole compounds is the main topic of this review including synthesis, SAR, and mechanism.

Keywords: Anticancer; Cancer; Cells apoptosis; Imidazole; SAR; Synthesis.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Heterocyclic Compounds* / chemical synthesis
  • Heterocyclic Compounds* / chemistry
  • Heterocyclic Compounds* / pharmacology
  • Humans
  • Imidazoles* / chemical synthesis
  • Imidazoles* / chemistry
  • Imidazoles* / pharmacology
  • Molecular Structure
  • Neoplasms / drug therapy
  • Structure-Activity Relationship

Substances

  • Imidazoles
  • Antineoplastic Agents
  • Heterocyclic Compounds
  • imidazole