New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

Publisher: Bentham Science Publishers

E-ISSN: 1875-6638|8|4|569-586

ISSN: 1573-4064

Source: Medicinal Chemistry, Vol.8, Iss.4, 2012-07, pp. : 569-586

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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.