1 Ocak 2018 Dergi makalesi Açık Erişim

Tuncbilek, Meral; Kucukdumlu, Asligul; Guven, Ebru Bilget; Altiparmak, Duygu; Cetin-Atalay, Rengul

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/35245</identifier>
  <creators>
    <creator>
      <creatorName>Tuncbilek, Meral</creatorName>
      <givenName>Meral</givenName>
      <familyName>Tuncbilek</familyName>
      <affiliation>Ankara Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06100 Ankara, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Kucukdumlu, Asligul</creatorName>
      <givenName>Asligul</givenName>
      <familyName>Kucukdumlu</familyName>
      <affiliation>Ankara Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06100 Ankara, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Guven, Ebru Bilget</creatorName>
      <givenName>Ebru Bilget</givenName>
      <familyName>Guven</familyName>
      <affiliation>Bilkent Univ, Dept Mol Biol &amp; Genet, TR-06800 Ankara, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Altiparmak, Duygu</creatorName>
      <givenName>Duygu</givenName>
      <familyName>Altiparmak</familyName>
      <affiliation>Ankara Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06100 Ankara, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Cetin-Atalay, Rengul</creatorName>
      <givenName>Rengul</givenName>
      <familyName>Cetin-Atalay</familyName>
      <affiliation>ODTU, Grad Sch Informat, Canc Syst Biol Lab, TR-06800 Ankara, Turkey</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Synthesis Of Novel 6-Substituted Amino-9-(Beta-D-Ribofuranosyl)Purine Analogs And Their Bioactivities On Human Epithelial Cancer Cells</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2018</publicationYear>
  <dates>
    <date dateType="Issued">2018-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/35245</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1016/j.bmcl.2017.12.070</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">New nucleoside derivatives with nitrogen substitution at the C-6 position were prepared and screened initially for their in vitro anticancer bioactivity against human epithelial cancer cells (liver Huh7, colon HCT116, breast MCF7) by the NCI-sulforhodamine B assay. N-6-(4-trifluoromethylphenyl) piperazine analog (27) exhibited promising cytotoxic activity. The compound 27 was more cytotoxic (IC50 = 1-4 mu M) than 5-FU, fludarabine on Huh7, HCT116 and MCF7 cell lines. The most potent nucleosides (11, 13, 16, 18, 19, 21, 27, 28) were further screened for their cytotoxicity in hepatocellular cancer cell lines. The compound 27 demonstrated the highest cytotoxic activity against Huh7, Mahlavu and FOCUS cells (IC50 = 1, 3 and 1 mu M respectively). Physicochemical properties, drug-likeness, and drug score profiles of the molecules showed that they are estimated to be orally bioavailable. The results pointed that the novel derivatives would be potential drug candidates. (C) 2018 Elsevier Ltd. All rights reserved.</description>
  </descriptions>
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