8-Aza-7,9-dideazaxanthine acyclic nucleoside phosphonate inhibitors of thymidine phosphorylase

3- and 8-(8-phosphonooctyl)-8-aza-7,9-dideazaxanthine, and 1,8-bis(8-aza-7,9-dideazaxanthin-8-yl)octane were prepared and found to inhibit thymidine phosphorylase from Escherichia coli, human recombinant TP expressed in V79, and TP purified from human placenta. The IC 50 values ranged from 3.5 to 27...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (2), p.652-654
Main Authors: Mařák, David, Otmar, Miroslav, Votruba, Ivan, Dračínský, Martin, Krečmerová, Marcela
Format: Article
Language:English
Subjects:
8-Aza-7,9-dideazaxanthine
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Escherichia coli
Escherichia coli - enzymology
Female
Humans
Nucleotide analog
Placenta
Placenta - enzymology
Pregnancy
Pyrimidinones - chemistry
Pyrimidinones - pharmacology
Pyrroles - chemistry
Pyrroles - pharmacology
Pyrrolo[3,4-d]pyrimidine
Recombinant Proteins - antagonists & inhibitors
Recombinant Proteins - metabolism
Structure-Activity Relationship
Thymidine Phosphorylase - antagonists & inhibitors
Thymidine Phosphorylase - metabolism
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Summary:3- and 8-(8-phosphonooctyl)-8-aza-7,9-dideazaxanthine, and 1,8-bis(8-aza-7,9-dideazaxanthin-8-yl)octane were prepared and found to inhibit thymidine phosphorylase from Escherichia coli, human recombinant TP expressed in V79, and TP purified from human placenta. The IC 50 values ranged from 3.5 to 27 μM.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.12.027