title: Effect of stilbene and chalcone scaffolds incorporation in clofibric acid on PPARα agonistic activity.
abstract: In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and trans-stilbene, chalcone, and other lipophilic groups were synthesized. They were evaluated for PPARα transactivation activity; all branched derivatives showed an increase of the transcriptional activity of receptor compared to the linear ones. Noteworthy, stilbene and benzophenone branched derivatives activated the PPARα better than clofibric acid.
authors: Letizia
authors: L
authors: Giampietro
authors: Alessandra
authors: A
authors: D'Angelo
authors: Antonella
authors: A
authors: Giancristofaro
authors: Alessandra
authors: A
authors: Ammazzalorso
authors: Barbara
authors: B
authors: De Filippis
authors: Mauro
authors: M
authors: Di Matteo
authors: Marialuigia
authors: M
authors: Fantacuzzi
authors: Pasquale
authors: P
authors: Linciano
authors: Cristina
authors: C
authors: Maccallini
authors: Dipartimento di Farmacia, Università di Chieti, via dei Vestini, 66100 Chieti, Italy. ramoroso@unich.it.
authors: Rosa
authors: R
authors: Amoroso
mesh_terms: D002460:Cell Line; D002599:Chalcone / Q000737:chemistry* / Q000494:pharmacology; D002995:Clofibric Acid / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D015533:Transcriptional Activation / Q000187:drug effects
chemical_list: D047493:PPAR alpha; D013267:Stilbenes; D002995:Clofibric Acid; D002599:Chalcone