| Autor: |
Yarim, Mine, Koksal, Meric, Schepmann, Dirk, Wuensch, Bernard |
| Přispěvatelé: |
Yarim, M., Koksal, M., Schepmann, D., Wünsch, B., Yeditepe Üniversitesi |
| Jazyk: |
angličtina |
| Rok vydání: |
2011 |
| Předmět: |
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| Popis: |
To investigate the molecular features involved in sigma (?) receptors binding, a series of compounds based on indole scaffolds were synthesized and their chemical structures were confirmed by 1H-NMR, IR, and elemental analysis. Their affinity toward ? 1 and ? 2 receptor subtypes was evaluated. 1-{[4-(2-phenylethyl)piperazin-1-yl]methyl}-3-methyl-1H-indole 3b had a high affinity to ? 1 receptors, while three compounds, 1-{3-[4-(substitutedphenyl)piperazin-1-yl]propyl}-1H-indole derivatives 4a-c had shown high affinity and selectivity for ? 2 receptors. Cytotoxicity of the compounds was demonstrated on cancer cell lines from liver (HUH7), breast (MCF7), and colon (HCT-116) cancer cell lines. Compound 1c (3-{[4-(3,4-dichlorobenzyl)piperazin-1-yl]methyl}-1H-indole) showed significant cell growth inhibitory activity on the selected cancer cell lines. © 2011 John Wiley & Sons A/S. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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