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Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines

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2020
Authors
Wittine, Karlo
Antolović, Roberto
Jelić, Dubravko
Bracanović, Sara
Cetina, Mario
Anđelković, Uroš
Wittine, Ozren
Kraljević Pavelić, Sandra
Vinter, Adrijana
Article (Published version)
,
Elsevier
Metadata
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Abstract
Furanocoumarins, particularly furo[3,2-c]coumarins, are found in many natural products. However, coumarins annulated to a thiophene ring have received scarce attention to date in the literature. Therefore, we synthesized 4-oxo-4H-thieno[3,2-c]chromene derivatives and tested in vitro their anti-inflammatory activity. Anti-inflammatory potential of the synthesized compounds (1, 2, 6–8, 9a–e and 10a–c) has been evaluated by measuring various pSTAT (signal transducer and activator of transcription) inhibition within the JAK (Janus-activated family kinase)/STAT signaling pathway. Ethyl 7-hydroxy-4-oxo-4H-thieno[3,2-c]chromene-2-carboxylate (7) showed best inhibition properties on pSTAT5 in GM-CSF (Granulocyte-macrophage colony-stimulating factor)-triggered PBMC assay, with IC50 value of 5.0 μM.
Keywords:
Thieno[3,2-c]chromene / Coumarin / Anti-inflammatory / Interleukin / Cytokine
Source:
Bioorganic & Medicinal Chemistry Letters, 2020, 30, 18, 127415-
Publisher:
  • Elsevier
Projects:
  • University of Rijeka research grant 13.11.1.1.11 (RISK “Development of University of Rijeka campus laboratory research infrastructure”)

DOI: 10.1016/j.bmcl.2020.127415

ISSN: 0960-894X

PubMed: 32717616

WoS: 000571824300011

Scopus: 2-s2.0-85088107865
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/3614
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