Literature DB >> 28544586

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

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.
© 2017 John Wiley & Sons A/S.

Entities:  

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

Mesh:

Substances:

Year:  2017        PMID: 28544586     DOI: 10.1111/cbdd.13026

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  7 in total

1.  Sulfonimide and Amide Derivatives as Novel PPARα Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies.

Authors:  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
Journal:  ACS Med Chem Lett       Date:  2020-03-03       Impact factor: 4.345

2.  Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies.

Authors:  Alessandra Ammazzalorso; Simone Carradori; Andrea Angeli; Atilla Akdemir; Barbara De Filippis; Marialuigia Fantacuzzi; Letizia Giampietro; Cristina Maccallini; Rosa Amoroso; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

3.  Screening of Benzimidazole-Based Anthelmintics and Their Enantiomers as Repurposed Drug Candidates in Cancer Therapy.

Authors:  Rosalba Florio; Simone Carradori; Serena Veschi; Davide Brocco; Teresa Di Genni; Roberto Cirilli; Adriano Casulli; Alessandro Cama; Laura De Lellis
Journal:  Pharmaceuticals (Basel)       Date:  2021-04-17

4.  Benzothiazole Derivatives Endowed with Antiproliferative Activity in Paraganglioma and Pancreatic Cancer Cells: Structure-Activity Relationship Studies and Target Prediction Analysis.

Authors:  Rosa Amoroso; Laura De Lellis; Rosalba Florio; Nazaret Moreno; Mariangela Agamennone; Barbara De Filippis; Letizia Giampietro; Cristina Maccallini; Inmaculada Fernández; Rocío Recio; Alessandro Cama; Marialuigia Fantacuzzi; Alessandra Ammazzalorso
Journal:  Pharmaceuticals (Basel)       Date:  2022-07-28

5.  Aberrant Expression of Peroxisome Proliferator-Activated Receptors in Colorectal Cancer and Their Association with Cancer Progression and Prognosis.

Authors:  Musa Yaghoubizadeh; Leila Pishkar; Gholam Basati
Journal:  Gastrointest Tumors       Date:  2019-11-01

6.  Effects of repurposed drug candidates nitroxoline and nelfinavir as single agents or in combination with erlotinib in pancreatic cancer cells.

Authors:  Serena Veschi; Laura De Lellis; Rosalba Florio; Paola Lanuti; Alberto Massucci; Nicola Tinari; Michele De Tursi; Pierluigi di Sebastiano; Marco Marchisio; Clara Natoli; Alessandro Cama
Journal:  J Exp Clin Cancer Res       Date:  2018-09-21

Review 7.  PPAR Ligands Induce Antiviral Effects Targeting Perturbed Lipid Metabolism during SARS-CoV-2, HCV, and HCMV Infection.

Authors:  Marialuigia Fantacuzzi; Rosa Amoroso; Alessandra Ammazzalorso
Journal:  Biology (Basel)       Date:  2022-01-11
  7 in total

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