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

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...

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Bibliographic Details
Published in:European journal of organic chemistry 2022-06, Vol.2022 (21), p.n/a
Main Authors: Grosjean, Félix, Cros‐Perrial, Emeline, Braka, Abdenour, Uttaro, Jean‐Pierre, Chaloin, Laurent, Jordheim, Lars Petter, Peyrottes, Suzanne, Mathé, Christophe
Format: Article
Language:English
Subjects:
5′-Ecto-nucleotidase
Adenosine
Biochemistry, Molecular Biology
Chemical Sciences
Cheminformatics
Enzymatic inhibitors
Immuno-oncology
Inhibitors
Life Sciences
Scaffolds
Structural Biology
Triazole derivatives
Triazoles
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Summary: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. Several series of substituted 1,4,5‐triazole derivatives bearing various aryls, alkyls and indoles groups were synthetized, as inhibitors of 5′‐ectonucleotidase CD73, and evaluated for their potential inhibitory effect on purified recombinant hCD73 enzyme and in cell‐based assays. Among them, some compounds were found to be potent enzymatic inhibitors at 10 μM.
ISSN:1434-193X
1099-0690
DOI:10.1002/ejoc.202101175