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Updated: Jul 14, 2026

HPLC-based Assay to Monitor Extracellular Nucleotide/Nucleoside Metabolism in Human Chronic Lymphocytic Leukemia Cells
Published on: July 20, 2016
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands
Jacob Ravn1, Katrine Qvortrup, Christoph Rosenbohm
1Santaris Pharma A/S, Bøge Alle 3, DK-2970 Hørsholm, Denmark. jra@santaris.com
Abstract:
We have prepared a series of adenosine analogs based on the bicyclo[2.2.1]heptane scaffold of locked nucleic acid (LNA) and tested them for both agonist and antagonist activity at the adenosine A(3) receptor. The design of these derivatives was based on the known A(3) agonist IB-MECA and related compounds. Modifications thus include the 5'-uronamides and N(6)-(3-iodobenzyl) derivatives. In this way we have prepared analogs of known A(3) agonists with the sugar ring restricted in an N-conformation. For comparison we have also prepared 2'-O-methyl derivatives of IB-MECA. The LNA nucleosides showed no agonist activity but some of them are potent antagonists. The 2'-O-methyl derivative of IB-MECA is an agonist with similar potency as the parent compound.
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