2. Academic Validation
  3. Synthesis, σ₁, σ₂-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes

Synthesis, σ₁, σ₂-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes

  • Bioorg Med Chem. 2012 May 15;20(10):3323-31. doi: 10.1016/j.bmc.2012.03.038.
Stefanos Riganas 1,  Ioannis Papanastasiou,  George B Foscolos,  Andrew Tsotinis,  Jean-Jacques Bourguignon,  Guillaume Serin,  Jean-François Mirjolet,  Kostas Dimas,  Vassilios N Kourafalos,  Andreas Eleutheriades,  Vassilios I Moutsos,  Humaira Khan,  Stavroula Georgakopoulou,  Angeliki Zaniou,  Margarita Prassa,  Maria Theodoropoulou,  Stavroula Pondiki,  Alexandre Vamvakides
Affiliations

Affiliation

  • 1 Faculty of Pharmacy, Department of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 157 71 Athens, Greece.
PMID: 22512908 DOI: 10.1016/j.bmc.2012.03.038
Abstract

The synthesis of N-{4-[a-(1-adamantyl)benzyl]phenyl}piperazines 2a-e is described. The in vitro antiproliferative activity of most compounds against main Cancer cell lines is significant. The σ(1), σ(2)-receptors and sodium channels binding affinity of compounds 2 were investigated. One of the most active analogs, 2a, had an interesting in vivo Anticancer profile against the BxPC-3 and Mia-Paca-2 pancreas Cancer cell lines with Caspase-3 activation, which was associated with an anagelsic activity against the neuropathic pain.

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