期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 18, 页码 5688-5693出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.07.031
关键词
N,O-nucleosides; Furopyrimidines; Sonogashira reaction; Antiviral activity; Cytotoxicity
资金
- Italian Ministry of Education, Universities, and Research (MIUR)
- University of Messina (Italy)
- University of Catania (Italy)
- Interuniversity Consortium for Innovative Methodologies and Processes for Synthesis (CINMPIS)
A series of modified N,O-nucleosides, characterized by the presence of a furopyrimidine moiety, has been synthesized by exploiting a Sonogashira cross coupling reaction of 1-isoxazolidiny1-5-iodouracil with alkynes, followed by treatment with Cul in refluxing TEA/MeOH mixture. The obtained compounds were screened against both RNA and DNA viruses. None of the compounds were endowed with antiviral activity at subtoxic concentrations. However, some of them were able to inhibit proliferation of MRC-5, Vero, BS-C-1 cells by 50% (CC50) at concentrations ranging from 0.7 to 62.5 mM. (C) 2013 Elsevier Ltd. All rights reserved.
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