Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 9, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127067
Keywords
Thiazolo[5,4-d]pyrimidine; Adenosine A(2A) receptor inverse agonists; CD73 inhibitors; Cancer immunotherapy; Antitumor agents
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Funding
- Universita degli Studi di Firenze
- Fondazione AIRC per la Ricerca sul Cancro (AIRC-MFAG) [21753]
- Universita degli Studi di Ferrara
- Natural Sciences and Engineering Research Council of Canada (NSERC) [RGPIN-2016-05867]
- Fonds de Recherche du Quebec - Sante (FRQS)
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico of Brazil (CNPq)
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Adenosine pathway, including its generating enzyme (CD73) and its receptors represents a key target for cancer immunotherapy. Here we aimed to search for novel compounds able to co-target the CD73 and the A(2A) adenosine receptor (A(2A) AR) as dual-blockers of adenosine generation and activity. The design project was to combine in the same molecule the thiazolo [5,4-d]pyrimidine core, an essential pharmacophoric feature to block the A(2A) AR, with a benzenesulfonamide group which is a characteristic group of CD73 inhibitors. Most of the reported compounds resulted in inverse agonists of the human (h) A(2A) AR endowed with high affinity, selectivity and potency. However they were weak inhibitors of CD73 enzyme. Nevertheless, this study can be considered as a starting point to develop more active compounds.
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