Abstract: 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-D-anomer exclusively. The in vitro antitumor effects of β-D-MPR and 6-methyl-purine-α-D- riboside (α-D-MPR) in five human tumor cell lines showed that β-D-MPR was highly active (IC 50 values ranging from 6 to 34 nM). α-D-MPR, although less active than β-D-MPR, ...