New adamantane derivatives with sigma affinity and antiproliferative activity
| Autor: | Andreas Eleutheriades, Vassilios N. Kourafalos, Athanasios Mantelas, Ioannis Papanastasiou, Alexandre Vamvakides, Stavroula Pondiki, Stavroula Georgakopoulou, Stefanos Riganas, Vassilios I. Moutsos, Kostas Dimas, George B. Foscolos, Maria Theodoropoulou, Prassa Margarita, Angeliki Zaniou, Andrew Tsotinis, Humaira Khan |
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| Rok vydání: | 2011 |
| Předmět: |
Male
Binding Sites Chemistry Sodium channel Adamantane Antineoplastic Agents Mice SCID Pharmacology In vitro Adamantane derivatives Mice Cell culture In vivo Cell Line Tumor Drug Design Neoplasms Drug Discovery Animals Humans Receptors sigma Female Cancer cell lines Binding site Receptor Cell Proliferation |
| Zdroj: | Medicinal chemistry (Shariqah (United Arab Emirates)). 8(4) |
| ISSN: | 1875-6638 |
| Popis: | 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. 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. |
| Databáze: | OpenAIRE |
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