2. Academic Validation
  3. New adamantane phenylalkylamines with σ-receptor binding affinity and anticancer activity, associated with putative antagonism of neuropathic pain

New adamantane phenylalkylamines with σ-receptor binding affinity and anticancer activity, associated with putative antagonism of neuropathic pain

  • J Med Chem. 2012 Nov 26;55(22):10241-61. doi: 10.1021/jm3013008.
Stefanos Riganas 1,  Ioannis Papanastasiou,  George B Foscolos,  Andrew Tsotinis,  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,  Athanasios Mantelas,  Stavroula Pondiki,  Alexandre Vamvakides
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15771 Athens, Greece.
PMID: 23094992 DOI: 10.1021/jm3013008
Abstract

The synthesis of the adamantane phenylalkylamines 2a-d, 3a-c, and 4a-e is described. These compounds exhibited significant antiproliferative activity, in vitro, against eight Cancer cell lines tested. The σ(1), σ(2), and Sodium Channel binding affinities of compounds 2a, 3a, 4a, and 4c-e were investigated. The most interesting analogue, 4a, exhibited significant in vivo Anticancer profile on pancreas, prostate, leukemia, and ovarian Cancer cell line xenografts together with Apoptosis and Caspase-3 activation. Inhibition of the Cancer cells cycle at the sub-G1 level was also obtained with 4a. Finally, encouraging results were observed with 4a in vivo on mice, suggesting putative antimetastatic and analgesic activities of this compound.

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