New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

作者：Riganas Stefanos; Papanastasiou Ioannis; Foscolos George B^*; Tsotinis Andrew; Dimas Kostas; Kourafalos Vassilios N; Eleutheriades Andreas; Moutsos Vassilios I; Khan Humaira; Margarita Prassa; Georgakopoulou Stavroula; Zaniou Angeliki; Theodoropoulou Maria; Mantelas Athanasios; Pondiki Stavroula; Vamvakides Alexandre

来源：Medicinal Chemistry, 2012, 8(4): 569-586.

DOI：10.2174/157340612801216201

• Diaryladamantanealkanamines
• synthesis
• sigma-receptors affinity
• sodium channels affinity
• anti-proliferative activity
• in vivo anticancer profile

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 sigma 1, sigma 2-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.

• 出版日期2012-7