Synthesis and Biological Evaluation of 9??Oxo??9H??indeno [1, 2??b] pyrazine??2, 3??dicarbonitrile Analogues as Potential Inhibitors of Deubiquitinating Enzymes

M Colombo, S Vallese, I Peretto, X Jacq…

Index: Colombo, Matteo; Vallese, Stefania; Peretto, Ilaria; Jacq, Xavier; Rain, Jean-Christophe; Colland, Frederic; Guedat, Philippe ChemMedChem, 2010 , vol. 5, # 4 p. 552 - 558

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Citation Number: 30

Abstract

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 ...