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.
TY - JOUR
AU - Wittine, Karlo
AU - Antolović, Roberto
AU - Jelić, Dubravko
AU - Bracanović, Sara
AU - Cetina, Mario
AU - Anđelković, Uroš
AU - Wittine, Ozren
AU - Kraljević Pavelić, Sandra
AU - Vinter, Adrijana
PY - 2020
UR - https://cer.ihtm.bg.ac.rs/handle/123456789/3614
AB - 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.
PB - Elsevier
T2 - Bioorganic & Medicinal Chemistry Letters
T1 - Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines
VL - 30
IS - 18
SP - 127415
DO - 10.1016/j.bmcl.2020.127415
ER -
@article{
author = "Wittine, Karlo and Antolović, Roberto and Jelić, Dubravko and Bracanović, Sara and Cetina, Mario and Anđelković, Uroš and Wittine, Ozren and Kraljević Pavelić, Sandra and Vinter, Adrijana",
year = "2020",
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.",
publisher = "Elsevier",
journal = "Bioorganic & Medicinal Chemistry Letters",
title = "Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines",
volume = "30",
number = "18",
pages = "127415",
doi = "10.1016/j.bmcl.2020.127415"
}
Wittine, K., Antolović, R., Jelić, D., Bracanović, S., Cetina, M., Anđelković, U., Wittine, O., Kraljević Pavelić, S.,& Vinter, A.. (2020). Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines. in Bioorganic & Medicinal Chemistry Letters
Elsevier., 30(18), 127415.
https://doi.org/10.1016/j.bmcl.2020.127415
Wittine K, Antolović R, Jelić D, Bracanović S, Cetina M, Anđelković U, Wittine O, Kraljević Pavelić S, Vinter A. Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines. in Bioorganic & Medicinal Chemistry Letters. 2020;30(18):127415.
doi:10.1016/j.bmcl.2020.127415 .
, 
