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Halogenated Rocaglate Derivatives: Pan-antiviral Agents against Hepatitis E Virus and Emerging Viruses.


ABSTRACT: 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.

SUBMITTER: Victoria C 

PROVIDER: S-EPMC10788925 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature

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Halogenated Rocaglate Derivatives: Pan-antiviral Agents against Hepatitis E Virus and Emerging Viruses.

Victoria Catherine C   Schulz Göran G   Klöhn Mara M   Weber Saskia S   Holicki Cora M CM   Brüggemann Yannick Y   Becker Miriam M   Gerold Gisa G   Eiden Martin M   Groschup Martin H MH   Steinmann Eike E   Kirschning Andreas A  

Journal of medicinal chemistry 20231221 1


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 activit  ...[more]

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