New Adamantane Phenylalkylamines with 蟽-Receptor Binding Affinity and Anticancer Activity, Associated with Putative Antagonism of Neuropathic Pain
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- 作者：Stefanos Riganas ; Ioannis Papanastasiou ; George B. Foscolos ; Andrew Tsotinis ; Guillaume Serin ; Jean-Fran莽ois Mirjolet ; Kostas Dimas ; Vassilios N. Kourafalos ; Andreas Eleutheriades ; Vassilios I. Moutsos ; Humaira Khan ; Stavroula Georgakopoulou ; Angeliki Zaniou ; Margarita Prassa ; Maria Theodoropoulou ; Athanasios Mantelas ; Stavroula Pondiki ; Alexandre Vamvakides
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：November 26, 2012
- 年：2012
- 卷：55
- 期：22
- 页码：10241-10261
- 全文大小：658K
- 年卷期：v.55,no.22(November 26, 2012)
- ISSN：1520-4804
文摘
The synthesis of the adamantane phenylalkylamines 2a鈥?b>d, 3a鈥?b>c, and 4a鈥?b>e is described. These compounds exhibited significant antiproliferative activity, in vitro, against eight cancer cell lines tested. The 蟽1, 蟽2, and sodium channel binding affinities of compounds 2a, 3a, 4a, and 4c鈥?b>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.