2. Academic Validation
  3. Dihydrithieno[2,3-b]naphto-4,9-dione analogues as anticancer agents: Synthesis and in cell pharmacological studies

Dihydrithieno[2,3-b]naphto-4,9-dione analogues as anticancer agents: Synthesis and in cell pharmacological studies

  • Eur J Med Chem. 2015 Sep 18:102:106-14. doi: 10.1016/j.ejmech.2015.07.044.
Alessia Bertamino 1,  Simona Musella 2,  Veronica Di Sarno 1,  Carmine Ostacolo 3,  Michele Manfra 4,  Daniela Vanacore 5,  Paola Stiuso 5,  Ettore Novellino 3,  Pietro Campiglia 1,  Isabel M Gomez-Monterrey 6
Affiliations

Affiliations

  • 1 Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
  • 2 Department of Pharmaceutical Sciences and Health Products, University of Messina, Viale Annunziata, 98168 Messina, Italy.
  • 3 Department of Pharmacy, University of Naples Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy.
  • 4 Department of Sciences, University of Basilicata, Via dell'Ateneo Lucano 10, 85100 Potenza, Italy.
  • 5 Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, Via Luigi De Crecchio 7, 80138 Naples, Italy.
  • 6 Department of Pharmacy, University of Naples Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy. Electronic address: imgomez@unina.it.
PMID: 26253231 DOI: 10.1016/j.ejmech.2015.07.044
Abstract

The synthesis of a series of highly functionalized DNTQ-based derivatives is described. In vitro, most of the compounds exerted a cytotoxic effect against several tumour cell lines comparable to or greater than that of doxorubicin. Here we demonstrate that compound 14, the less cardiotoxic compound of this series, induced cell differentiation and was distributed mainly in the cytoplasm in the human glioblastoma LN229 cell line. Moreover, compound 14 reduced both cellular glucose uptake and serine/threonine kinase Akt expression, and triggered cell Apoptosis. These findings suggest that highly functionalized DTNQ-based derivatives are promising pharmacological tools for the study of human solid tumours.

Keywords

Anti-tumor agents; Apoptosis; Cellular glucose uptake; Quinone derivatives.

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