Document Report Card

ID: ALA1154633

Journal: J Med Chem

Title: Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor.

Authors: Volpini R, Buccioni M, Dal Ben D, Lambertucci C, Lammi C, Marucci G, Ramadori AT, Klotz KN, Cristalli G.

Abstract: A new series of 2-aralkynyl-N(6)-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a new Eu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA(3)R with N(6)-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA(1)R and AA(2A)R. Furthermore, the new nucleosides showed to be full agonists, the N(6)-methyl-2-(2-pyridinyl)ethynylMECA (13) being the most potent in the series.

CiteXplore: 19839592

DOI: 10.1021/jm900754g