Benzimidazole Derivatives as Kinase Inhibitors

Author(s): Laura Garuti, Marinella Roberti, Giovanni Bottegoni.

Journal Name: Current Medicinal Chemistry

Volume 21 , Issue 20 , 2014

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.

Keywords: ATP-competitive, benzimidazole, biological activity, kinase inhibition, multi-target inhibitor, SAR, selectivity.

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 21
ISSUE: 20
Year: 2014
Page: [2284 - 2298]
Pages: 15
DOI: 10.2174/0929867321666140217105714
Price: $58

Article Metrics

PDF: 38