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Synthesis and Studies of Potential Inhibitors of CD73 Based on a Triazole Scaffold
Journal article   Open access   Peer reviewed

Synthesis and Studies of Potential Inhibitors of CD73 Based on a Triazole Scaffold

Félix Grosjean, Emeline Cros-Perrial, Abdenour Braka, Jean-Pierre Uttaro, Laurent Chaloin, Lars Petter Jordheim, Suzanne Peyrottes and Christophe Mathé
European Journal of Organic Chemistry, Vol.2022(21)
07/06/2022

Abstract

5’-Ecto-nucleotidase · Enzymatic inhibitors · Triazole derivatives · Immuno-oncology
The ecto-5′-nucleotidase CD73 is involved in the production of immunosuppressive adenosine in the tumoral microenvironment and recently became a validated target in immuno-oncology. To avoid formation of CD73-produced adenosine, several series of potential inhibitors of the target enzyme based on a triazole scaffold were synthetized and evaluated on recombinant purified hCD73 and in cell-based assays.
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