TY  - JOUR
AU  - Useini, Liridona
AU  - Komazec, Teodora
AU  - Laube, Markus
AU  - Lönnecke, Peter
AU  - Schädlich, Jonas
AU  - Mijatović, Sanja
AU  - Maksimović-Ivanić, Danijela
AU  - Pietzsch, Jens
AU  - Hey-Hawkins, Evamarie
PY  - 2023
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/5826
AB  - Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used
therapeutics against pain, fever, and inflammation; additionally, antitumor
properties are reported. NSAIDs reduce the synthesis of prostaglandins by
inhibiting the cyclooxygenase (COX) isoforms COX-1 and COX-2. As
nonselective inhibition is associated with off-target effects, strategies to
achieve selectivity for the clinically preferred isoform COX-2 are of high
interest. The modification of NSAIDs using carborane clusters as phenyl
mimetics is reported to alter the selectivity profile through size exclusion.
Inspired by these findings, isonimesulide and its carborane derivatives are
prepared. The biological screening shows that the carborane containing
compounds exhibit a stronger antitumor potential compared to nimesulide
and isonimesulide. Furthermore, the replacement of the phenyl ring of
isonimesulide with a carborane moiety resulted in a shift of the COX activity
from nonactive to COX-active compounds.
PB  - Hoboken: Wiley
T2  - Advanced Therapeutics
T1  - Isonimesulide and Its Carborane Analogues as Isoform-Selective COX Inhibitors and Antitumor Agents
DO  - 10.1002/adtp.202300117
SP  - 2300117
ER  - 

@article{
author = "Useini, Liridona and Komazec, Teodora and Laube, Markus and Lönnecke, Peter and Schädlich, Jonas and Mijatović, Sanja and Maksimović-Ivanić, Danijela and Pietzsch, Jens and Hey-Hawkins, Evamarie",
year = "2023",
abstract = "Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used
therapeutics against pain, fever, and inflammation; additionally, antitumor
properties are reported. NSAIDs reduce the synthesis of prostaglandins by
inhibiting the cyclooxygenase (COX) isoforms COX-1 and COX-2. As
nonselective inhibition is associated with off-target effects, strategies to
achieve selectivity for the clinically preferred isoform COX-2 are of high
interest. The modification of NSAIDs using carborane clusters as phenyl
mimetics is reported to alter the selectivity profile through size exclusion.
Inspired by these findings, isonimesulide and its carborane derivatives are
prepared. The biological screening shows that the carborane containing
compounds exhibit a stronger antitumor potential compared to nimesulide
and isonimesulide. Furthermore, the replacement of the phenyl ring of
isonimesulide with a carborane moiety resulted in a shift of the COX activity
from nonactive to COX-active compounds.",
publisher = "Hoboken: Wiley",
journal = "Advanced Therapeutics",
title = "Isonimesulide and Its Carborane Analogues as Isoform-Selective COX Inhibitors and Antitumor Agents",
doi = "10.1002/adtp.202300117",
pages = "2300117"
}

Useini, L., Komazec, T., Laube, M., Lönnecke, P., Schädlich, J., Mijatović, S., Maksimović-Ivanić, D., Pietzsch, J.,& Hey-Hawkins, E.. (2023). Isonimesulide and Its Carborane Analogues as Isoform-Selective COX Inhibitors and Antitumor Agents. in Advanced Therapeutics
Hoboken: Wiley., 2300117.
https://doi.org/10.1002/adtp.202300117

Useini L, Komazec T, Laube M, Lönnecke P, Schädlich J, Mijatović S, Maksimović-Ivanić D, Pietzsch J, Hey-Hawkins E. Isonimesulide and Its Carborane Analogues as Isoform-Selective COX Inhibitors and Antitumor Agents. in Advanced Therapeutics. 2023;:2300117.
doi:10.1002/adtp.202300117 .

Useini, Liridona, Komazec, Teodora, Laube, Markus, Lönnecke, Peter, Schädlich, Jonas, Mijatović, Sanja, Maksimović-Ivanić, Danijela, Pietzsch, Jens, Hey-Hawkins, Evamarie, "Isonimesulide and Its Carborane Analogues as Isoform-Selective COX Inhibitors and Antitumor Agents" in Advanced Therapeutics (2023):2300117,
https://doi.org/10.1002/adtp.202300117 . .