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Halogenated rocaglate derivatives: pan-antiviral agents against hepatitis E virus and emerging viruses
Institute of Organic Chemistry, Leibniz University Hannover, Schneiderberg 1B, Hannover, Germany.
Institute of Organic Chemistry, Leibniz University Hannover, Schneiderberg 1B, Hannover, Germany.
Department of Molecular and Medical Virology, Ruhr-University Bochum, Bochum, Germany.
Federal Research Institute in Animal Health (FLI), Südufer 10, Insel Riems, Greifswald, Germany.
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2024 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 67, no 1, p. 289-321Article in journal (Refereed) Published
Abstract [en]

The synthesis of a library of halogenated rocaglate derivatives belonging to the flavagline class of natural products, of which silvestrol is the most prominent example, is reported. Their antiviral activity and cytotoxicity profile against a wide range of pathogenic viruses, including hepatitis E, Chikungunya, Rift Valley Fever virus and SARS-CoV-2, were determined. The incorporation of halogen substituents at positions 4′, 6 and 8 was shown to have a significant effect on the antiviral activity of rocaglates, some of which even showed enhanced activity compared to CR-31-B and silvestrol.

Place, publisher, year, edition, pages
American Chemical Society (ACS), 2024. Vol. 67, no 1, p. 289-321
National Category
Medicinal Chemistry Microbiology in the medical area
Identifiers
URN: urn:nbn:se:umu:diva-220155DOI: 10.1021/acs.jmedchem.3c01357ISI: 001141760200001PubMedID: 38127656Scopus ID: 2-s2.0-85181007683OAI: oai:DiVA.org:umu-220155DiVA, id: diva2:1836825
Available from: 2024-02-12 Created: 2024-02-12 Last updated: 2024-02-12Bibliographically approved

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Gerold, Gisa

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Wallenberg Centre for Molecular Medicine at Umeå University (WCMM)Section of Virology
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