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The synthesis of a series of novel C-linked nucleotide triphosphates is reported. These exhibit excellent agonist potency and selectivity for the P2Y2 receptor with a number of examples having EC50 values below 10 nM. Representative compounds from the N-linked and C-linked series showed enhanced metabolic stability compared with that of the natural ligand UTP.

Original publication

DOI

10.1016/j.bmcl.2006.10.038

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

15/01/2007

Volume

17

Pages

558 - 561

Keywords

Cell Line, Tumor, Chromatography, Liquid, Humans, Indicators and Reagents, Ligands, Magnetic Resonance Spectroscopy, Mass Spectrometry, Nucleotides, Purinergic P2 Receptor Agonists, Receptors, Purinergic P2Y2, Recombinant Proteins, Spectrophotometry, Ultraviolet, Uridine Triphosphate