Sulfonimide and Amide Derivatives as Novel PPARα Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies
Alessandra Ammazzalorso, Isabella Bruno, Rosalba Florio, Laura De Lellis, Antonio Laghezza, Carmen Cerchia, Barbara De Filippis, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Paolo Tortorella, Serena Veschi, Fulvio Loiodice, Antonio Lavecchia, Alessandro Cama, Rosa Amoroso
Abstract
lower than commercial PPARα antagonist GW6471 and a negligible toxicity on normal fibroblast cells. Docking studies were also performed to elucidate the binding mode of these compounds and to help interpretation of SAR data.
Topics & Concepts
Docking (animal)AntagonistAmideChemistryAgonistAntagonismMoietyStereochemistryTransactivationViability assayDU145Peroxisome proliferator-activated receptorReceptorPharmacologyBiochemistryCellCancer cellBiologyTranscription factorInternal medicineMedicineCancerNursingGeneLNCaPPeroxisome Proliferator-Activated ReceptorsPeptidase Inhibition and AnalysisProtein Degradation and Inhibitors