1 Ocak 2011 Dergi makalesi Açık Erişim

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

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/22863</identifier>
  <creators>
    <creator>
      <creatorName>Yarim, Mine</creatorName>
      <givenName>Mine</givenName>
      <familyName>Yarim</familyName>
      <affiliation>Yeditepe Univ, Dept Pharmaceut Chem, Fac Pharm, TR-34755 Istanbul, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Koksal, Meric</creatorName>
      <givenName>Meric</givenName>
      <familyName>Koksal</familyName>
      <affiliation>Yeditepe Univ, Dept Pharmaceut Chem, Fac Pharm, TR-34755 Istanbul, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Schepmann, Dirk</creatorName>
      <givenName>Dirk</givenName>
      <familyName>Schepmann</familyName>
      <affiliation>Inst Pharmazeut &amp; Med Chem, D-48149 Munster, Germany</affiliation>
    </creator>
    <creator>
      <creatorName>Wuensch, Bernard</creatorName>
      <givenName>Bernard</givenName>
      <familyName>Wuensch</familyName>
      <affiliation>Inst Pharmazeut &amp; Med Chem, D-48149 Munster, Germany</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Synthesis And In Vitro Evaluation Of Novel Indole-Based Sigma Receptors Ligands</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2011</publicationYear>
  <dates>
    <date dateType="Issued">2011-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/22863</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1111/j.1747-0285.2011.01215.x</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://www.opendefinition.org/licenses/cc-by">Creative Commons Attribution</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="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.</description>
  </descriptions>
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