1 Ocak 2011 Dergi makalesi Açık Erişim

Yarim, Mine; Koksal, Meric; Schepmann, Dirk; Wuensch, Bernard

Citation Style Language JSON

{
  "DOI": "10.1111/j.1747-0285.2011.01215.x", 
  "abstract": "To investigate the molecular features involved in sigma (sigma) receptors binding, a series of compounds based on indole scaffolds were synthesized and their chemical structures were confirmed by H-1-NMR, IR, and elemental analysis. Their affinity toward sigma(1) and sigma(2) receptor subtypes was evaluated. 1-{[4-(2-phenylethyl)piperazin-1-yl]methyl}-3-methyl-1H-indole 3b had a high affinity to sigma(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 sigma(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.", 
  "author": [
    {
      "family": "Yarim", 
      "given": " Mine"
    }, 
    {
      "family": "Koksal", 
      "given": " Meric"
    }, 
    {
      "family": "Schepmann", 
      "given": " Dirk"
    }, 
    {
      "family": "Wuensch", 
      "given": " Bernard"
    }
  ], 
  "container_title": "CHEMICAL BIOLOGY & DRUG DESIGN", 
  "id": "22863", 
  "issue": "5", 
  "issued": {
    "date-parts": [
      [
        2011, 
        1, 
        1
      ]
    ]
  }, 
  "page": "869-875", 
  "title": "Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands", 
  "type": "article-journal", 
  "volume": "78"
}