Synthesis of adenosine analogues with indole moiety as human adenosine A3 receptor ligands.

ABSTRACT: Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A1, A2A, A2B and A3, which belong to the G-protein-coupled receptor superfamily. The human A3AR (hA3AR) subtype is implicated in several cytoprotective functions. Therefore, hA3AR modulators, and in particular agonists, are sought for their potential application as anti-inflammatory, anti-cancer and cardioprotective agents. Here, we prepared novel adenosine derivatives with indole moiety as hA3AR ligands. According to the biological assay, we found that 2-substituents 11 were critical structural determinants for A3AR ligands (Ki = 111 nM). The observed structure-affinity relationships of this class of ligands were also exhaustively rationalized using the molec

SUBMITTER: Xia Y 

PROVIDER: S-EPMC5830761 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature