2. Academic Validation
  3. Synthesis of a resveratrol analogue with high ceramide-mediated proapoptotic activity on human breast cancer cells

Synthesis of a resveratrol analogue with high ceramide-mediated proapoptotic activity on human breast cancer cells

  • J Med Chem. 2005 Nov 3;48(22):6783-6. doi: 10.1021/jm050528k.
Filippo Minutolo 1,  Giusy Sala,  Annalisa Bagnacani,  Simone Bertini,  Isabella Carboni,  Giorgio Placanica,  Giovanni Prota,  Simona Rapposelli,  Nicoletta Sacchi,  Marco Macchia,  Riccardo Ghidoni
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Sciences, University of Pisa, via Bonanno 6, 56126 Pisa, Italy.
PMID: 16250636 DOI: 10.1021/jm050528k
Abstract

Resveratrol, a natural product with a stilbene structure, exerts profound proapoptotic activity in human Cancer cells, by triggering the accumulation of ceramide, a bioactive sphingolipid. We studied the biological effects of seven methoxylated and/or naphthalene-based resveratrol analogues and compared these compounds with resveratrol with the objective to identify an analogue with higher ceramide-mediated proapoptotic activity relative to resveratrol. Here we show that the compound with three hydroxyls and a naphthalene ring is the most effective in triggering Apoptosis coupled to the induction of endogenous ceramide in human Cancer cells.

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