D-4′-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor

Abstract

4′-Thionucleoside derivatives as potent and selective A3 adenosine receptor agonists were synthesized, starting from D-gulono-γ- lactone via D-thioribosyl acetate as a key intermediate, among which the 2· chloro-N6-methyladenosine-5′-methyluronamide showed the most potent and selective binding affinity (Ki = 0.28 ± 0.09 nM) at the human A3 adenosine receptor. Copyright © Taylor & Francis, Inc.