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Molecules 2005, 10(8), 1015-1020; doi:10.3390/10081015
Article

Improved Synthesis of β-D-6-Methylpurine Riboside and Antitumor Effects of the β-D- and α-D-Anomers

Jr. 1,* , 2, 2, 2 and 2
1 D’Youville College, Department of Math and Natural Sciences, USA 2 Grace Cancer Drug Center, Roswell Park Cancer Institute, USA
* Author to whom correspondence should be addressed.
Received: 10 December 2004 / Revised: 27 May 2005 / Accepted: 26 May 2005 / Published: 31 August 2005
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Abstract

6-Methylpurine-β-D-riboside (β-D-MPR) has been synthesized by coupling6-methylpurine and 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribose using conditions that producethe 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 washighly active (IC50 values ranging from 6 to 34 nM). α-D-MPR, although less active than β-D-MPR, also exhibited significant antitumor effects (IC50 values ranging from 1.47 to 4.83"µ"M).
Keywords: 6-Methylpurine-β-D-riboside; 6-methylpurine-α-D-riboside; antitumor activity; synthesis 6-Methylpurine-β-D-riboside; 6-methylpurine-α-D-riboside; antitumor activity; synthesis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Marasco, C., Jr.; Pera, P.; Spiess, A.; Bernacki, R.; Sufrin, J. Improved Synthesis of β-D-6-Methylpurine Riboside and Antitumor Effects of the β-D- and α-D-Anomers. Molecules 2005, 10, 1015-1020.

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