Recent advances of benzimidazole as anticancer agents

Chem Biol Drug Des. 2023 Aug;102(2):357-376. doi: 10.1111/cbdd.14236. Epub 2023 Apr 3.

Abstract

Cancer is the second leading cause of death globally, with 9.6 million deaths yearly. As a life-threatening disease, it necessitates the emergence of new therapies. Resistance to current chemotherapies drives scientists to develop new medications that will eventually be accessible. Because heterocycles are so common in biological substances, compounds play a big part in the variety of medications that have been developed. The "Master Key" is the benzimidazole nucleus, which consists of a six-membered benzene ring fused with a five-membered imidazole/imidazoline ring, which is an azapyrrole. One of the five-membered aromatic nitrogen heterocycles identified in American therapies that have been approved by the Food and Drug Administration (FDA). Our results show that benzimidazole's broad therapeutic spectrum is due to its structural isosteres with purine, which improves hydrogen bonding, electrostatic interactions with topoisomerase complexes, intercalation with DNA, and other functions. It also enhances protein and nucleic acid inhibition, tubulin microtubule degeneration, apoptosis, DNA fragmentation, and other functions. Additionally, readers for designing the more recent benzimidazole analogues as prospective cancer treatments.

Keywords: PARP; androgen receptor; benzimidazole; cancer targets; topoisomerase; tubulin inhibitors; tyrosine kinase.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology
  • DNA
  • Pharmaceutical Preparations

Substances

  • Antineoplastic Agents
  • Pharmaceutical Preparations
  • Benzimidazoles
  • DNA