New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

Title:New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

Volume: 8 Issue: 4

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

Affiliation:

Keywords: Diaryladamantanealkanamines, synthesis, sigma-receptors affinity, sodium channels affinity, anti-proliferative activity, in vivo anticancer profile, diarylbutylamines, hydrophobic adamantane, ovarian, xenograft

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.

Cite this article as:

Riganas Stefanos, Papanastasiou Ioannis, B. Foscolos George, Tsotinis Andrew, Dimas Kostas, N. Kourafalos Vassilios, Eleutheriades Andreas, I. Moutsos Vassilios, Khan Humaira, Margarita Prassa, Georgakopoulou Stavroula, Zaniou Angeliki, Theodoropoulou Maria, Mantelas Athanasios, Pondiki Stavroula and Vamvakides Alexandre, New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity, Medicinal Chemistry 2012; 8 (4) . https://dx.doi.org/10.2174/157340612801216201