title: Pyrimidine acyclic nucleoside phosphonates and phosphorylated analogs. Part 2. Syntheses and investigation of their inhibitory effects towards human thymidine phosphorylase.
abstract: Various methods were used in the syntheses of a number of pyrimidine acyclic nucleoside phosphonates and their derivatives such as a nucleophilic fluorination, Suzuki-Miyaura coupling reactions and phosphorylation. These new compounds were further investigated for their potential biological activity. Based on results obtained the ability to inhibit human thymidine phosphorylase some of them was found.
authors.affiliation: Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Centre for New Antivirals and Antineoplastics (IOCB), Flemingovo nám. 2,166 10, Prague, Czech Republic. pomeisl@uochb.cas.cz
authors.forename: Karel
authors.initials: K
authors.lastname: Pomeisl
authors.forename: Anonín
authors.initials: A
authors.lastname: Holý
authors.forename: Ivan
authors.initials: I
authors.lastname: Votruba
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D063065:Organophosphonates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010766:Phosphorylation; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors*; D013941:Thymine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: C541639:1-(3-fluoro-2-(phosphonomethoxy)propyl)thymine; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D063065:Organophosphonates; D013939:Thymidine Phosphorylase; D013941:Thymine