Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes
- ChemMedChem. 2010 Apr 6;5(4):552-8. doi: 10.1002/cmdc.200900409.
Affiliations
- 1. NiKem Research, via Zambeletti 25, 20021 Baranzate, Milan, Italy. [email protected]
PMID: 20186914
DOI: 10.1002/cmdc.200900409
Abstract
High-throughput screening highlighted 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile (1) as an active inhibitor of ubiquitin-specific proteases (USPs), a family of hydrolytic Enzymes involved in the removal of ubiquitin from protein substrates. The chemical behavior of compound 1 was examined. Moreover, the synthesis and in vitro evaluation of new compounds, analogues of 1, led to the identification of potent and selective inhibitors of the deubiquitinating enzyme USP8.
Products
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Cat. No.Product NameDescriptionTargetResearch Area
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target: DeubiquitinaseResearch Areas: Cancer
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target: DeubiquitinaseResearch Areas: Neurological Disease; Inflammation/Immunology; Infection; Cardiovascular Disease; Cancer
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target: DeubiquitinaseResearch Areas: Cancer
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