Anti-influenza virus activity of benzo[d]thiazoles that target heat shock protein 90
Copyright © 2020 Elsevier Inc. All rights reserved..
Seasonal or pandemic influenza virus infections are a worldwide health problem requiring antiviral therapy. Since virus resistance to the established neuraminidase inhibitors and novel polymerase inhibitors is growing, new drug targets are needed. Heat shock protein 90 (Hsp90) is associated with several aspects of the influenza virus life cycle, and is considered a relevant host cell target. We report here on a series of benzo[d]thiazole and 4,5,6,7-tetrahydrobenzo[d]thiazole derivatives with robust and selective activities against influenza A (H1N1, H3N2) and influenza B viruses. Two compounds, 1 and 4, have low micromolar EC50 values and show high binding affinities for Hsp90, which suggests that inhibition of Hsp90 is the mechanism underlying their antiviral effects. These compounds represent suitable scaffolds for designing novel Hsp90 inhibitors with favourable activities against influenza virus.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:98 |
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| Enthalten in: |
Bioorganic chemistry - 98(2020) vom: 01. Mai, Seite 103733 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Lamut, Andraž [VerfasserIn] |
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| Links: |
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| Themen: |
Antiviral Agents |
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| Anmerkungen: |
Date Completed 24.02.2021 Date Revised 24.02.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bioorg.2020.103733 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Seasonal or pandemic influenza virus infections are a worldwide health problem requiring antiviral therapy. Since virus resistance to the established neuraminidase inhibitors and novel polymerase inhibitors is growing, new drug targets are needed. Heat shock protein 90 (Hsp90) is associated with several aspects of the influenza virus life cycle, and is considered a relevant host cell target. We report here on a series of benzo[d]thiazole and 4,5,6,7-tetrahydrobenzo[d]thiazole derivatives with robust and selective activities against influenza A (H1N1, H3N2) and influenza B viruses. Two compounds, 1 and 4, have low micromolar EC50 values and show high binding affinities for Hsp90, which suggests that inhibition of Hsp90 is the mechanism underlying their antiviral effects. These compounds represent suitable scaffolds for designing novel Hsp90 inhibitors with favourable activities against influenza virus | ||
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| 650 | 4 | |a Antiviral agent | |
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| 700 | 1 | |a Gjorgjieva, Marina |e verfasserin |4 aut | |
| 700 | 1 | |a Naesens, Lieve |e verfasserin |4 aut | |
| 700 | 1 | |a Liekens, Sandra |e verfasserin |4 aut | |
| 700 | 1 | |a Lillsunde, Katja-Emilia |e verfasserin |4 aut | |
| 700 | 1 | |a Tammela, Päivi |e verfasserin |4 aut | |
| 700 | 1 | |a Kikelj, Danijel |e verfasserin |4 aut | |
| 700 | 1 | |a Tomašič, Tihomir |e verfasserin |4 aut | |
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