title: Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
abstract: We report on a series of novel 5,6-disubstituted uracils with significant inhibitory activity against human and Escherichia coli thymidine phosphorylases. Bis-uracil conjugates were identified as the most potent inhibitors of TPs in this study.
authors.affiliation: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 166 10 Prague 6, Czech Republic. nencka@uochb.cas.cz
authors.forename: Radim
authors.initials: R
authors.lastname: Nencka
authors.forename: Ivan
authors.initials: I
authors.lastname: Votruba
authors.forename: Hubert
authors.initials: H
authors.lastname: Hrebabecký
authors.forename: Eva
authors.initials: E
authors.lastname: Tloust'ová
authors.forename: Kveta
authors.initials: K
authors.lastname: Horská
authors.forename: Milena
authors.initials: M
authors.lastname: Masojídková
authors.forename: Antonín
authors.initials: A
authors.lastname: Holý
mesh_terms: D000588:Amines / Q000737:chemistry; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000588:Amines; D004791:Enzyme Inhibitors; D014498:Uracil; D013939:Thymidine Phosphorylase