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Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands

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


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<oai_dc:dc xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xsi:schemaLocation="http://www.openarchives.org/OAI/2.0/oai_dc/ http://www.openarchives.org/OAI/2.0/oai_dc.xsd">
  <dc:creator>Yarim, Mine</dc:creator>
  <dc:creator>Koksal, Meric</dc:creator>
  <dc:creator>Schepmann, Dirk</dc:creator>
  <dc:creator>Wuensch, Bernard</dc:creator>
  <dc:date>2011-01-01</dc:date>
  <dc: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.</dc:description>
  <dc:identifier>https://aperta.ulakbim.gov.trrecord/22863</dc:identifier>
  <dc:identifier>oai:zenodo.org:22863</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>http://www.opendefinition.org/licenses/cc-by</dc:rights>
  <dc:source>CHEMICAL BIOLOGY &amp; DRUG DESIGN 78(5) 869-875</dc:source>
  <dc:title>Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands</dc:title>
  <dc:type>info:eu-repo/semantics/article</dc:type>
  <dc:type>publication-article</dc:type>
</oai_dc:dc>
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