Benzimidazole derivatives as kinase inhibitors
| Autor: | Marinella Roberti, Laura Garuti, Giovanni Bottegoni |
|---|---|
| Přispěvatelé: | Garuti L, Roberti M, Bottegoni G. |
| Rok vydání: | 2013 |
| Předmět: |
Models
Molecular Benzimidazole Stereochemistry biological activity Biology ATP-competitive benzimidazole kinase inhibition multi-target inhibitor SAR selectivity HETEROCYCLES Biochemistry Cell Line chemistry.chemical_compound Structure-Activity Relationship Protein structure Biological property Drug Discovery Structure–activity relationship Humans Protein Kinase Inhibitors Pharmacology chemistry.chemical_classification Kinase Organic Chemistry Biological activity Protein Structure Tertiary Enzyme chemistry Cell culture Molecular Medicine Benzimidazoles |
| Zdroj: | Current medicinal chemistry. 21(20) |
| ISSN: | 1875-533X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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