Synthetic and Medicinal Perspective of 1,2,4-Triazole as Anticancer Agents

Chem Biodivers. 2022 Nov;19(11):e202200679. doi: 10.1002/cbdv.202200679. Epub 2022 Nov 4.

Abstract

Cancer is still one of the leading causes of death worldwide. Many researchers are working to design and develop heterocyclic-based drugs with the potential to treat cancer at various stages. There is always an unmet need to discover new anticancer drugs to treat different types of cancer. Based on literature reports, it was evident that hybrid 1,2,4-triazoles exhibit a wide spectrum of biological potential (particularly potent anticancer activity), as compared to the corresponding monocyclic compounds. In this review, we summarized fused/hybrid 1,2,4-triazole and poly-functionalized 1,2,4-triazoles as anticancer agents. Triazole may be fused with other heterocyclic scaffolds like pyrimidine, pyridine, piperidine, quinoxaline, quinazoline, thiadiazine, indole, phthalazine etc. A clear explanation of the method of synthesis, structure-activity relationship, and in vitro results plus the inhibitory concentration of new molecules are focused on in this review article.

Keywords: 1,2,4-triazole; anticancer; cytotoxicity; heterocycles; structure-activity relationship.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Humans
  • Molecular Structure
  • Neoplasms* / drug therapy
  • Structure-Activity Relationship
  • Triazoles* / pharmacology
  • Triazoles* / therapeutic use

Substances

  • 1,2,4-triazole
  • Antineoplastic Agents
  • Triazoles