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. 2023 Mar 1;18(5):e202200583.
doi: 10.1002/cmdc.202200583. Epub 2023 Jan 18.

Carborane Analogues of Fenoprofen Exhibit Improved Antitumor Activity

Liridona Useini  1 , Marija Mojić  2 , Markus Laube  3 , Peter Lönnecke  1 , Sanja Mijatović  2 , Danijela Maksimović-Ivanić  2 , Jens Pietzsch  3   4 , Evamarie Hey-Hawkins  1
Affiliations

Carborane Analogues of Fenoprofen Exhibit Improved Antitumor Activity

Liridona Useini et al. ChemMedChem. .

Abstract

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: COX inhibitors; Carborane; cancer; drug design; fenoprofen.

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