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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

Author(s): 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 and Alexandre Vamvakides

Volume 8 , Issue 4 , 2012

Page: [569 - 586] Pages: 18

DOI: 10.2174/157340612801216201

Price: $65


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

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