Počet záznamů: 1

Use of Pd-catalyzed Suzuki-Miyaura coupling reaction in the rapid synthesis of 5-aryl-6-(phosphonomethoxy)uracils and evaluation of their inhibitory effect towards human thymidine phosphorylase

  1. 1.
    0330906 - UOCHB-X 2010 RIV GB eng J - Článek v odborném periodiku
    Pomeisl, Karel - Holý, Antonín - Pohl, Radek - Horská, Květoslava
    Use of Pd-catalyzed Suzuki-Miyaura coupling reaction in the rapid synthesis of 5-aryl-6-(phosphonomethoxy)uracils and evaluation of their inhibitory effect towards human thymidine phosphorylase.
    Tetrahedron. Roč. 65, č. 41 (2009), s. 8486-8492 ISSN 0040-4020
    Grant CEP: GA MŠk 1M0508; GA AV ČR 1QS400550501
    Výzkumný záměr: CEZ:AV0Z40550506
    Klíčová slova: acyclic nucleoside phosphonates * Suzuki-Miyaura reaction * thymidine phosphorylase * human thymidine phosphorylase
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 3.219, rok: 2009

    A number of new 5-aryl substituted pyrimidine acyclic nucleoside phosphonates were synthesized and tested for their ability to inhibit human TP. Their rapid synthesis using Pd-catalyzed Suzuki-Miyaura coupling reactions of various arylboronic acids with 5-bromo-4-(phosphonomethoxy)-2,6-dibutoxypyrimidine was succesfully applied. For a series of 5-aryl-6-phosphonomethoxyuracils, an increased inhibitory effect was determined. This effect is supported by the results found for 4-fluorophenyl (KidThd = 4.89 ±0.62) and 3-nitrophenyl (KidThd = 3.98 ±0.46) substituents.
    Trvalý link: http://hdl.handle.net/11104/0176579