Synthesis, σ1, σ2-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes

What is it about?

The synthesis of N-{4-[a-(1-adamantyl)benzyl]phenyl}piperazines 2a–e is described. The in vitro antiproliferative activity of most compounds against main cancer cell lines is significant. The σ1, σ2-receptors and sodium channels binding affinity of compounds 2 were investigated. One of the most active analogs, 2a, had an interesting in vivo anticancer profile against the BxPC-3 and Mia-Paca-2 pancreas cancer cell lines with caspase-3 activation, which was associated with an anagelsic activity against the neuropathic pain.

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