| Literature DB >> 28544586 |
Alessandra Ammazzalorso1, Laura De Lellis2,3, Rosalba Florio2,3, Isabella Bruno1, Barbara De Filippis1, Marialuigia Fantacuzzi1, Letizia Giampietro1, Cristina Maccallini1, Silvia Perconti3, Fabio Verginelli2,3, Alessandro Cama2,3, Rosa Amoroso1.
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.Entities:
Keywords: CPT1A expression; PPAR antagonist; antitumor agents; cytotoxicity; sulfonamides
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Year: 2017 PMID: 28544586 DOI: 10.1111/cbdd.13026
Source DB: PubMed Journal: Chem Biol Drug Des ISSN: 1747-0277 Impact factor: 2.817