Conjugable A₃ adenosine receptor antagonists for the development of functionalized ligands and their use in fluorescent probes.

ABSTRACT: Compounds able to simultaneously bind a biological target and be conjugated to a second specific moiety are attractive tools for the development of multi-purpose ligands useful as multi-target ligands, receptor probes or drug delivery systems, with both therapeutic and diagnostic applications. The human A₃ adenosine receptor is a G protein-coupled receptor involved in many physio-pathological conditions, e.g. cancer and inflammation, thus representing a promising research target. In this work, two series of conjugable hA₃AR antagonists, based on the pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine nucleus, were developed. The introduction of an aromatic ring at the 5 position of the scaffold, before (phenylacetamido moiety) or after (1,2,3-triazole obtained by click ch

SUBMITTER: Federico S 

PROVIDER: S-EPMC7199890 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature