title: Benzimidazole derivatives as kinase inhibitors.
abstract: 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.
authors.forename: Laura
authors.initials: L
authors.lastname: Garuti
authors.forename: Marinella
authors.initials: M
authors.lastname: Roberti
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, via Belmeloro 6, I-40126 Bologna, Italy. laura.garuti@unibo.it.
authors.forename: Giovanni
authors.initials: G
authors.lastname: Bottegoni
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D017434:Protein Structure, Tertiary; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; C031000:benzimidazole