Počet záznamů: 1

Synthesis and biological evaluation of acyclic nucleotide analogues with a furo[2,3-d]pyrimidin-2(3H)-one base

  1. 1.
    0345964 - UOCHB-X 2011 RIV CA eng J - Článek v odborném periodiku
    Janeba, Zlatko - Holý, Antonín - Pohl, Radek - Snoeck, R. - Andrei, G. - De Clercq, E. - Balzarini, J.
    Synthesis and biological evaluation of acyclic nucleotide analogues with a furo[2,3-d]pyrimidin-2(3H)-one base.
    Canadian Journal of Chemistry. Roč. 88, č. 7 (2010), s. 628-638 ISSN 0008-4042
    Grant CEP: GA MŠk 1M0508
    Výzkumný záměr: CEZ:AV0Z40550506
    Klíčová slova: acyclic nucleoside phosphonates * Sonogashira reaction * intramolecular cyclization
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 1.374, rok: 2010

    A novel series of 2-(phosphonomethoxy)ethyl (PME) substituted furo[2,3-d]pyrimidin-2(3H)-ones with potential anti-VZV and/or anti-HCMV activity was synthesized. The target acyclic nucleotide analogues were prepared by Sonogashira coupling of protected 5-iodo-1-[2-(phosphonomethoxy)ethyl]uracil with various 1-alkynes, followed by in situ Cu(I)-promoted intramolecular cyclization and standard removal of the isopropyl ester groups. None of the prepared analogues were active at subtoxic concentrations against VZV thymidine kinase competent (TK+), VZV thymidine kinase deficient (TK–), or HCMV.
    Trvalý link: http://hdl.handle.net/11104/0187118