New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

Le résumé fourni par la source

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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