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Chem Biol Drug Des. 2017 Nov;90(5):1029-1035. doi: 10.1111/cbdd.13026. Epub 2017 Jul 19.

Cytotoxic effect of a family of peroxisome proliferator-activated receptor antagonists in colorectal and pancreatic cancer cell lines.

Author information

1
Unità di Chimica Farmaceutica, Dipartimento di Farmacia, Università "G. d'Annunzio", Chieti, Italy.
2
Unità di Patologia Generale, Dipartimento di Farmacia, Università "G. d'Annunzio", Chieti, Italy.
3
Aging Research Center (Ce.S.I.), Università "G. d'Annunzio", Chieti, Italy.

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.

KEYWORDS:

CPT1A expression; PPAR antagonist; antitumor agents; cytotoxicity; sulfonamides

PMID:
28544586
DOI:
10.1111/cbdd.13026
[Indexed for MEDLINE]

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