Synthesis and Studies of Potential Inhibitors of CD73 Based on a Triazole Scaffold. Issue 21 (9th December 2021)

• Record Type: Journal Article
• Authors: Grosjean, Félix; Cros‐Perrial, Emeline; Braka, Abdenour; Uttaro, Jean‐Pierre; Chaloin, Laurent; Jordheim, Lars Petter; Peyrottes, Suzanne; Mathé, Christophe
• Is Part Of: European journal of organic chemistry. Volume 2022:Issue 21(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2021-12-09
• Subjects: 5′-Ecto-nucleotidase -- Enzymatic inhibitors -- Triazole derivatives -- Immuno-oncology; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1002/ejoc.202101175
• Languages: English
• ISSNs: 1434-193X

Abstract

Abstract: 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 h CD73 and in cell‐based assays. Abstract : 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 h CD73 enzyme and in cell‐based assays. Among them, some compounds were found to be potent enzymatic inhibitors at 10 μM.