Carborane Analogues of Fenoprofen Exhibit Improved Antitumor Activity
2023
Download 🢃
Authors:
Useini, LiridonaMojić, Marija
Laube, Markus
Lönnecke, Peter
Mijatović, Sanja
Maksimović-Ivanić, Danijela
Pietzsch, Jens
Hey‐Hawkins, Evamarie
Document Type:
Article (Published version)
Metadata
Show full item recordAbstract:
Fenoprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID) against rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis and gout. Like other NSAIDs, fenoprofen inhibits the synthesis of prostaglandins by blocking both cyclooxygenase (COX) isoforms, COX-1 the “house-keeping” enzyme and COX-2 the induced isoform from pathological stimuli. Unselective inhibition of both COX isoforms results in many side effects, but off-target effects have also been reported. The steric modifications of the drugs could afford the desired COX-2 selectivity. Furthermore, NSAIDs have shown promising cytotoxic properties. The structural modification of fenoprofen using bulky dicarba-closo-dodecaborane(12) (carborane) clusters and the biological evaluation of the carborane analogues for COX inhibition and antitumor potential showed that the carborane analogues exhibit stronger antitumor potential compared to their respective aryl-based compounds.
Keywords:
cancer; Carborane; COX inhibitors; drug design; fenoprofenSource:
ChemMedChem, 2023, 18, 5, e202200583-Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200007 (University of Belgrade, Institute for Biological Research 'Siniša Stanković') (RS-MESTD-inst-2020-200007)
- Deutscher Akademischer Austauschdienst 57381412
- Deutsche Forschungsgemeinschaft He 1376/54‐1, PI‐304/7‐1
DOI: 10.1002/cmdc.202200583
ISSN: 1860-7179
PubMed: 36583943
WoS: 000914767400001
Scopus: 2-s2.0-85146469898
URI
https://onlinelibrary.wiley.com/doi/10.1002/cmdc.202200583http://radar.ibiss.bg.ac.rs/handle/123456789/5432