Halogenated Rocaglate Derivatives

Pan-antiviral Agents against Hepatitis E Virus and Emerging Viruses

verfasst von

Catherine Victoria, Göran Schulz, Mara Klöhn, Saskia Weber, Cora M. Holicki, Yannick Brüggemann, Miriam Becker, Gisa Gerold, Martin Eiden, Martin H. Groschup, Eike Steinmann, Andreas Kirschning

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.

Organisationseinheit(en)

Institut für Organische Chemie

Externe Organisation(en)

Ruhr-Universität Bochum
Stiftung Tierärztliche Hochschule Hannover
Universität Umeå
Friedrich-Loeffler-Institut (FLI)

Typ

Artikel

Journal

Journal of medicinal chemistry

Band

67

Seiten

289-321

Anzahl der Seiten

33

ISSN

0022-2623

Publikationsdatum

11.01.2024

Publikationsstatus

Veröffentlicht

Peer-reviewed

Ja

ASJC Scopus Sachgebiete

Molekularmedizin, Wirkstoffforschung

Ziele für nachhaltige Entwicklung

SDG 3 – Gute Gesundheit und Wohlergehen

Elektronische Version(en)

https://doi.org/10.1021/acs.jmedchem.3c01357 (Zugang: Offen)