102933-75-5Relevant academic research and scientific papers
New adamantane derivatives with sigma affinity and antiproliferative activity
Riganas, Stefanos,Papanastasiou, Ioannis,Foscolos, George B.,Tsotinis, Andrew,Dimas, Kostas,Kourafalos, Vassilios N.,Eleutheriades, Andreas,Moutsos, Vassilios I.,Khan, Humaira,Margarita, Prassa,Georgakopoulou, Stavroula,Zaniou, Angeliki,Theodoropoulou, Maria,Mantelas, Athanasios,Pondiki, Stavroula,Vamvakides, Alexandre
experimental part, p. 569 - 586 (2012/09/08)
The synthesis of 4-(1-adamantyl)-4,4-diarylbutylamines 1, 5-(1-adamantyl)-5,5-diarylpentylamines 2 and 6-(1-adamantyl)-6,6- diarylhexylamines 3 is described and the σ1, σ2-receptors and sodium channels binding affinity of compounds 1 were investigated. Th
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.
