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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Benzimidazole Derivatives as Kinase Inhibitors

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

Volume 21, Issue 20, 2014

Page: [2284 - 2298] Pages: 15

DOI: 10.2174/0929867321666140217105714

Price: $65


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.

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