1 Ocak 2011 Dergi makalesi Açık Erişim

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

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{
  "@context": "https://schema.org/", 
  "@id": 22863, 
  "@type": "ScholarlyArticle", 
  "creator": [
    {
      "@type": "Person", 
      "affiliation": "Yeditepe Univ, Dept Pharmaceut Chem, Fac Pharm, TR-34755 Istanbul, Turkey", 
      "name": "Yarim, Mine"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Yeditepe Univ, Dept Pharmaceut Chem, Fac Pharm, TR-34755 Istanbul, Turkey", 
      "name": "Koksal, Meric"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Inst Pharmazeut & Med Chem, D-48149 Munster, Germany", 
      "name": "Schepmann, Dirk"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Inst Pharmazeut & Med Chem, D-48149 Munster, Germany", 
      "name": "Wuensch, Bernard"
    }
  ], 
  "datePublished": "2011-01-01", 
  "description": "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.", 
  "headline": "Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands", 
  "identifier": 22863, 
  "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", 
  "license": "http://www.opendefinition.org/licenses/cc-by", 
  "name": "Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands", 
  "url": "https://aperta.ulakbim.gov.tr/record/22863"
}