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Improved Synthesis of beta-D-6-Methylpurine Riboside and Antitumor Effects of the beta-D- and alpha-D-Anomers

Canio J. Marasco

6-Methylpurine-β-D-riboside (β-D-MPR) has been synthesized by coupling 6-methylpurine and 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribose using conditions that produce the β-Danomer exclusively. The in vitro antitumor effects of β-D-MPR and 6-methylpurine-α-Driboside (α-D-MPR) in five human tumor cell lines showed that β-D-MPR was highly active (IC50 values ranging from 6 to 34 nM).