Cytotoxic effect of a family of peroxisome proliferator‐activated receptor antagonists in colorectal and pancreatic cancer cell lines. (19th July 2017)

• Record Type: Journal Article
• Authors: Ammazzalorso, Alessandra; De Lellis, Laura; Florio, Rosalba; Bruno, Isabella; De Filippis, Barbara; Fantacuzzi, Marialuigia; Giampietro, Letizia; Maccallini, Cristina; Perconti, Silvia; Verginelli, Fabio; Cama, Alessandro; Amoroso, Rosa
• Is Part Of: Chemical biology & drug design. Volume 90:Number 5(2017)
• Page Start: 1029
• Page End: 1035
• Publication Date: 2017-07-19
• Subjects: antitumor agents -- CPT1A expression -- cytotoxicity -- PPAR antagonist -- sulfonamides; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.13026
• Languages: English
• ISSNs: 1747-0277

Abstract

Abstract : Recent studies report an interesting role of peroxisome proliferator‐activated receptor (PPAR) antagonists in different tumor models, being these compounds able to perturb metabolism and viability in cancer cells. In this work, the identification of a novel PPAR antagonist, showing inhibitory activity on PPARα and a weaker antagonism on PPARγ, is described. The activity of this compound and of a series of chemical analogues was investigated in selected tumor cell lines, expressing both PPARα and PPARγ. Data obtained show a dose‐dependent cytotoxic effect of the novel PPAR antagonist in colorectal and pancreatic cancer models. Abstract : In this work, the identification of a novel PPAR antagonist, showing inhibitory activity on PPARα and a weaker antagonism on PPARγ, is described. The activity of this compound and of a series of chemical analogues was investigated in selected tumor cell lines, expressing both PPARα and PPARγ. Data obtained show a dose‐dependent cytotoxic effect of the novel antagonist in colorectal and pancreatic cancer models.