engleski

Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines

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.

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

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