Details
| Original language | English |
|---|---|
| Pages (from-to) | 289-321 |
| Number of pages | 33 |
| Journal | Journal of medicinal chemistry |
| Volume | 67 |
| Issue number | 1 |
| Early online date | 21 Dec 2023 |
| Publication status | Published - 11 Jan 2024 |
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.
ASJC Scopus subject areas
- Biochemistry, Genetics and Molecular Biology(all)
- Molecular Medicine
- Pharmacology, Toxicology and Pharmaceutics(all)
- Drug Discovery
Sustainable Development Goals
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In: Journal of medicinal chemistry, Vol. 67, No. 1, 11.01.2024, p. 289-321.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Halogenated Rocaglate Derivatives
T2 - Pan-antiviral Agents against Hepatitis E Virus and Emerging Viruses
AU - Victoria, Catherine
AU - Schulz, Göran
AU - Klöhn, Mara
AU - Weber, Saskia
AU - Holicki, Cora M.
AU - Brüggemann, Yannick
AU - Becker, Miriam
AU - Gerold, Gisa
AU - Eiden, Martin
AU - Groschup, Martin H.
AU - Steinmann, Eike
AU - Kirschning, Andreas
N1 - Funding Information: E.S. was supported by the German Federal Ministry of Health (ZMVI1-2518FSB705) and a grant of the German Centre for Infection Diseases (DZIF). E.S., M.H.G. and A.K. were supported by the German Ministry of Education and Research (BMBF, project SILVIR: 16GW0202). G.G. received funding from the Lower Saxony Ministry of Science and Culture (15-76251-1-2/23 (511/2023)).
PY - 2024/1/11
Y1 - 2024/1/11
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85181007683&partnerID=8YFLogxK
U2 - 10.1021/acs.jmedchem.3c01357
DO - 10.1021/acs.jmedchem.3c01357
M3 - Article
C2 - 38127656
AN - SCOPUS:85181007683
VL - 67
SP - 289
EP - 321
JO - Journal of medicinal chemistry
JF - Journal of medicinal chemistry
SN - 0022-2623
IS - 1
ER -