New Adamantane Derivatives with Sigma Affinity and Antiproliferative Activity

被引:19
作者
Riganas, Stefanos [1 ,3 ]
Papanastasiou, Ioannis [1 ]
Foscolos, George B. [1 ]
Tsotinis, Andrew [1 ]
Dimas, Kostas [2 ]
Kourafalos, Vassilios N. [3 ]
Eleutheriades, Andreas [3 ]
Moutsos, Vassilios I. [3 ]
Khan, Humaira [3 ]
Margarita, Prassa [3 ]
Georgakopoulou, Stavroula [3 ]
Zaniou, Angeliki [3 ]
Theodoropoulou, Maria [3 ]
Mantelas, Athanasios [3 ]
Pondiki, Stavroula [3 ]
Vamvakides, Alexandre [3 ]
机构
[1] Univ Athens, Dept Pharmaceut Chem, Fac Pharm, Athens 15771, Greece
[2] FBRAA, Div Pharmacol, Athens 11527, Greece
[3] Anavex Life Sci, Athens 15351, Greece
关键词
Diaryladamantanealkanamines; synthesis; sigma-receptors affinity; sodium channels affinity; anti-proliferative activity; in vivo anticancer profile; GATED SODIUM-CHANNELS; IN-VITRO; CANCER-CELLS; LIPID RAFTS; TUMOR; RECEPTORS; ANTAGONISTS; INHIBITION; AGONISTS; DRUGS;
D O I
10.2174/157340612801216201
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 sigma 1, sigma 2-receptors and sodium channels binding affinity of compounds 1 were investigated. The in vitro activity of compounds 1, 2 and 3 against main cancer cell lines is significant. One of the most active analogs, 1a, had an interesting in vivo anticancer profile against the ovarian cancer cell line IGROV-1, which was associated with an anagelsic activity against the neuropathic pain induced by the main anticancer drugs.
引用
收藏
页码:569 / 586
页数:18
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