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  Medicinal Chemistry

Volume 8 Issue 4
ISSN: 1573-4064

 
   All Titles

New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity
pp.569-586 (18) Authors: Stefanos Riganas, Ioannis Papanastasiou, George B. Foscolos, Andrew Tsotinis, Kostas Dimas, Vassilios N. Kourafalos, Andreas Eleutheriades, Vassilios I. Moutsos, Humaira Khan, Prassa Margarita, Stavroula Georgakopoulou, Angeliki Zaniou, Maria Theodoropoulou, Athanasios Mantelas, Stavroula Pondiki, Alexandre Vamvakides
 
Abstract:

The synthesis of 4-(1-adamantyl)-4,4-diarylbutylamines 1, 5-(1-adamantyl)-5,5-diarylpentylamines 2 and 6-(1-adamantyl)-6,6-diarylhexylamines 3 is described and the σ1, σ2-receptors and sodium channels binding affinity of compounds 1 were investigated. The in vitro activity of compounds 1, 2 and 3 against main cancer cell lines is significant. One of the most active analogs, 1a, had an interesting in vivo anticancer profile against the ovarian cancer cell line IGROV-1, which was associated with an anagelsic activity against the neuropathic pain induced by the main anticancer drugs.

Keywords: Diaryladamantanealkanamines, synthesis, sigma-receptors affinity, sodium channels affinity, anti-proliferative activity, in vivo anticancer profile, diarylbutylamines, hydrophobic adamantane, ovarian, xenograft
Affiliation: Panepistimioupoli-Zografou, 157 71 Athens, Greece.

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