CER - Central Repository
Institute of Chemistry, Technology and Metallurgy
    • English
    • Српски
    • Српски (Serbia)
  • English 
    • English
    • Serbian (Cyrillic)
    • Serbian (Latin)
  • Login
View Item 
  •   CER
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
  •   CER
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

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 record
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.
Keywords:
Thieno[3,2-c]chromene / Coumarin / Anti-inflammatory / Interleukin / Cytokine
Source:
Bioorganic & Medicinal Chemistry Letters, 2020, 30, 18, 127415-
Publisher:
  • Elsevier
Funding / 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

WoS: 000571824300011

Scopus: 2-s2.0-85088107865
[ Google Scholar ]
3
2
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/3614
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
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 .
Wittine, Karlo, Antolović, Roberto, Jelić, Dubravko, Bracanović, Sara, Cetina, Mario, Anđelković, Uroš, Wittine, Ozren, Kraljević Pavelić, Sandra, Vinter, Adrijana, "Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines" in Bioorganic & Medicinal Chemistry Letters, 30, no. 18 (2020):127415,
https://doi.org/10.1016/j.bmcl.2020.127415 . .

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

re3dataOpenAIRERCUB
 

 

All of DSpaceInstitutions/communitiesAuthorsTitlesSubjectsThis institutionAuthorsTitlesSubjects

Statistics

View Usage Statistics

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

re3dataOpenAIRERCUB