Faculty of Pharmacy, Department of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 157 71 Athens, Greece.
Bioorg Med Chem. 2012 May 15;20(10):3323-31. doi: 10.1016/j.bmc.2012.03.038. Epub 2012 Mar 24.
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 σ(1), σ(2)-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.
描述了 N-｛4-[a-（1-金刚烷基）苄基｝哌嗪｝2a-e 的合成。大多数化合物对主要癌细胞系的体外抗增殖活性均具有显著作用。研究了化合物 2 的 σ（1）、σ（2）-受体和钠通道结合亲和力。最活跃的类似物之一 2a 对 BxPC-3 和 Mia-Paca-2 胰腺癌细胞系具有有趣的体内抗癌特性，可激活 caspase-3，同时具有抗神经病理性疼痛的作用。
