title: 8-Aza-7,9-dideazaxanthine acyclic nucleoside phosphonate inhibitors of thymidine phosphorylase.
abstract: 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 27μM.
authors.affiliation: Institute of Organic Chemistry and Biochemistry, v.v.i., Gilead Sciences & IOCB Research Center, Academy of Sciences of the Czech Republic, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.
authors.forename: David
authors.initials: D
authors.lastname: Mařák
authors.forename: Miroslav
authors.initials: M
authors.lastname: Otmar
authors.forename: Ivan
authors.initials: I
authors.lastname: Votruba
authors.forename: Martin
authors.initials: M
authors.lastname: Dračínský
authors.forename: Marcela
authors.initials: M
authors.lastname: Krečmerová
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D004926:Escherichia coli / Q000201:enzymology; D005260:Female; D006801:Humans; D010920:Placenta / Q000201:enzymology; D011247:Pregnancy; D011744:Pyrimidinones / Q000737:chemistry* / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D011744:Pyrimidinones; D011758:Pyrroles; D011994:Recombinant Proteins; D013939:Thymidine Phosphorylase