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

来源：

MEDICINAL CHEMISTRY | 2012年 / 8卷 / 04期

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

页码：569 / 586

页数：18

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