Benzimidazole derivatives as kinase inhibitors

Laura Garuti*, Marinella Roberti, Giovanni Bottegoni

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)


Benzimidazole is a common kinase inhibitor scaffold and benzimidazole-based compounds interact with enzymes by multiple binding modes. In some cases, the benzimidazole acts as part of the hinge-binding motif, in others it has a scaffolding role without evidence for direct hinge binding. Several of these compounds are ATP-competitive inhibitors and show high selectivity by exploiting unique structural properties that distinguish one kinase from the majority of other kinases. However, the high specificity for a single target is not always sufficient. Thus another approach, called multi-target therapy, has been developed over the last few years. The simultaneous inhibition of various kinases may be useful because the disease is attacked at several relevant targets. Moreover, if a kinase becomes drug-resistant, a multitargeted drug can act on the other kinases. Some benzimidazole derivatives are multi-target inhibitors. In this article benzimidazole inhibitors are reported with their mechanisms of action, structure-activity relationship (SAR) and biological properties.

Original languageEnglish
Pages (from-to)2284-2298
Number of pages15
JournalCurrent medicinal chemistry
Issue number20
Publication statusPublished - 1 Jan 2014


  • ATP-competitive
  • Benzimidazole
  • Biological activity
  • Kinase inhibition
  • Multi-target inhibitor
  • SAR
  • Selectivity

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Medicine(all)


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