Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines.
Basic Information
ID: ALA4665715
Journal: Bioorg Med Chem Lett
Title: Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines.
Authors: Wittine K,Antolović R,Jelić D,Bracanović S,Cetina M,Andjelkovic U,Wittine O,Kraljević Pavelić S,Vinter A
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 IC value of 5.0 µM.
CiteXplore: 32717616
DOI: 10.1016/j.bmcl.2020.127415
Patent ID: ┄