Anti-influenza virus activity of benzo[d]thiazoles that target heat shock protein 90

Andraž Lamut, Marina Gjorgjieva, Lieve Naesens, Sandra Liekens, Katja-Emilia Lillsunde, Päivi Tammela, Danijel Kikelj, Tihomir Tomašič

Forskningsoutput: TidskriftsbidragArtikelVetenskapligPeer review

Sammanfattning

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.
Originalspråkengelska
Artikelnummer103733
TidskriftBioorganic Chemistry
Volym98
Antal sidor8
ISSN0045-2068
DOI
StatusPublicerad - maj 2020
MoE-publikationstypA1 Tidskriftsartikel-refererad

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  • 317 Farmaci
  • 116 Kemi
  • 1182 Biokemi, cell- och molekylärbiologi

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