Halogenated Rocaglate Derivatives

Pan-antiviral Agents against Hepatitis E Virus and Emerging Viruses

authored by

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.

Organisation(s)

Institute of Organic Chemistry

External Organisation(s)

Ruhr-Universität Bochum
University of Veterinary Medicine of Hannover, Foundation
Umea University
Friedrich Loeffler Institute (FLI)

Type

Article

Journal

Journal of medicinal chemistry

Volume

67

Pages

289-321

No. of pages

33

ISSN

0022-2623

Publication date

11.01.2024

Publication status

Published

Peer reviewed

Yes

ASJC Scopus subject areas

Molecular Medicine, Drug Discovery

Sustainable Development Goals

SDG 3 - Good Health and Well-being

Electronic version(s)

https://doi.org/10.1021/acs.jmedchem.3c01357 (Access: Open)