4.7 Article

Synthesis of a novel ester of hydroxytyrosol and alpha-lipoic acid exhibiting an antiproliferative effect on human colon cancer HT-29 cells

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 1, Pages 439-446

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.10.028

Keywords

Hydroxytyrosol; alpha-Lipoic acid; Antiproliferative activity; Human colon cancer HT-29 cell line; 2-Iodoxybenzoic acid (IBX)

Funding

  1. Ministero dell'Universita e della Ricerca Scientifica e Tecnologica
  2. University of Tuscia, Viterbo (Italy)

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A novel ester of hydroxytyrosol and alpha-lipoic acid was synthesized in satisfactory yield by original and simple procedures and evaluated about its antiproliferative activity on the human colorectal adenocarcinoma HT-29 cell line. The compound exhibited a cell growth inhibitory activity significantly more potent than the corresponding parent natural compounds, very likely due to the induction of cell cycle arrest in the G2/M phase. These data suggest that the novel ester might exert a more effective antitumour activity than hydroxytyrosol and alpha-lipoic acid. (C) 2010 Elsevier Masson SAS. All rights reserved.

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