New Adamantane Phenylalkylamines with σ-Receptor Binding Affinity and Anticancer Activity, Associated with Putative Antagonism of Neuropathic Pain

What is it about?

The synthesis of the adamantane phenylalkylamines 2a−d, 3a−c, and 4a−e is described. These compounds exhibited significant antiproliferative activity, in vitro, against eight cancer cell lines tested. The σ1, σ2, and sodium channel binding affinities of compounds 2a, 3a, 4a, and 4c−e were investigated. The most interesting analogue, 4a, exhibited significant in vivo anticancer profile on pancreas, prostate, leukemia, and ovarian cancer cell line xenografts together with apoptosis and caspase-3 activation. Inhibition of the cancer cells cycle at the sub-G1 level was also obtained with 4a. Finally, encouraging results were observed with 4a in vivo on mice, suggesting putative antimetastatic and analgesic activities of this compound.

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