Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines
Authorized Users Only
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
Show full item recordAbstract
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 / CytokineSource:
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