Naslov
Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines

Autori
Wittine, Karlo ; Antolović, Roberto ; Jelić, Dubravko ; Bracanović, Sara ; Cetina, Mario ; Andjelkovic, Uroš ; Wittine, Ozren ; Kraljević Pavelić, Sandra ; Vinter, Adrijana

Izvornik
Bioorganic & medicinal chemistry letters (0960-894X) 30 (2020), 18; 127415, 5

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Thieno[3, 2-c]chromene ; Coumarin ; Anti-inflammatory ; Interleukin ; Cytokine ; JAK/STAT

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Interdisciplinarne prirodne znanosti

POVEZANOST RADA