Carboranyl Analogues of Mefenamic Acid and Their Biological Evaluation.
2022
Autori:
Useini, LiridonaMojić, Marija
Laube, Markus
Lönnecke, Peter
Dahme, Jonas
Sárosi, Menyhárt B.
Mijatović, Sanja
Maksimović-Ivanić, Danijela
Pietzsch, Jens
Hey-Hawkins, Evamarie
Tip dokumenta:
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt:
Mefenamic acid represents a widely used nonsteroidal anti-inflammatory drug (NSAID) to treat the pain of postoperative surgery and heavy menstrual bleeding. Like other NSAIDs, mefenamic acid inhibits the synthesis of prostaglandins by nonselectively blocking cyclooxygenase (COX) isoforms COX-1 and COX-2. For the improved selectivity of the drug and, therefore, reduced related side effects, the carborane analogues of mefenamic acid were evaluated. The ortho-, meta-, and para-carborane derivatives were synthesized in three steps: halogenation of the respective cluster, followed by a Pd-catalyzed B-N coupling and hydrolysis of the nitrile derivatives under acidic conditions. The COX inhibitory activity and cytotoxicity for different cancer cell lines revealed that the carborane analogues have stronger antitumor potential compared to their parent organic compound.
Izvor:
ACS Omega, 2022, 7, 28, 24282-24291Finansiranje / projekti:
- Ministarstvo nauke, tehnološkog razvoja i inovacija Republike Srbije, institucionalno finansiranje - 200007 (Univerzitet u Beogradu, Institut za biološka istraživanja 'Siniša Stanković') (RS-MESTD-inst-2020-200007)
- Deutscher Akademischer Austausch Dienst (DAAD) - 57381412
- German Research Foundation (DFG) HE 1376/54-1 PI 304/7-1
DOI: 10.1021/acsomega.2c01523
ISSN: 2470-1343
PubMed: 35874202
WoS: 000823305000001
Scopus: 2-s2.0-85134806986
URI
https://pubs.acs.org/doi/10.1021/acsomega.2c01523http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9301635
http://radar.ibiss.bg.ac.rs/handle/123456789/5075