1410789-76-2Relevant academic research and scientific papers
New adamantane phenylalkylamines with σ-receptor binding affinity and anticancer activity, associated with putative antagonism of neuropathic pain
Riganas, Stefanos,Papanastasiou, Ioannis,Foscolos, George B.,Tsotinis, Andrew,Serin, Guillaume,Mirjolet, Jean-Fran?ois,Dimas, Kostas,Kourafalos, Vassilios N.,Eleutheriades, Andreas,Moutsos, Vassilios I.,Khan, Humaira,Georgakopoulou, Stavroula,Zaniou, Angeliki,Prassa, Margarita,Theodoropoulou, Maria,Mantelas, Athanasios,Pondiki, Stavroula,Vamvakides, Alexandre
, p. 10241 - 10261 (2013/01/16)
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.
