Novel PPARα Antagonists Bearing Stilbene or Bioisosteres Endowed with Antiproliferative Effects in Cancer Cell Lines

Image

Peroxisome Proliferator-Activated Receptors (PPARs) have been widely studied in the last decades, and they attracted the attention of scientists as promising therapeutic targets. Intensive efforts by researchers produced a wide panel of drugs targeting the three PPAR subtypes (PPARα, PPARβ, PPARγ) able to modulate important metabolic functions. PPAR activation is involved in several physiologic pathways, as lipid and glucose metabolism, insulin sensitivity, energy homeostasis, and cell differentiation. Fibrates and thiazolidinediones, respectively synthetic PPARα and PPARγ agonists, are currently used for the treatment of hyperlipidemia and hyperglycemia, in patients affected by type 2 diabetes and metabolic syndrome[