1 Ocak 2022 Dergi makalesi Açık Erişim

Uygun, Meltem Tan; Amudi, Karina; Turacli, Irem Dogan; Menges, Nurettin

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/231626</identifier>
  <creators>
    <creator>
      <creatorName>Uygun, Meltem Tan</creatorName>
      <givenName>Meltem Tan</givenName>
      <familyName>Uygun</familyName>
    </creator>
    <creator>
      <creatorName>Amudi, Karina</creatorName>
      <givenName>Karina</givenName>
      <familyName>Amudi</familyName>
    </creator>
    <creator>
      <creatorName>Turacli, Irem Dogan</creatorName>
      <givenName>Irem Dogan</givenName>
      <familyName>Turacli</familyName>
      <affiliation>Ufuk Univ, Fac Med, Dept Med Biol, TR-06520 Ankara, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Menges, Nurettin</creatorName>
      <givenName>Nurettin</givenName>
      <familyName>Menges</familyName>
    </creator>
  </creators>
  <titles>
    <title>A New Synthetic Approach For Pyrazolo[1,5-A]Pyrazine-4(5H)-One Derivatives And Their Antiproliferative Effects On Lung Adenocarcinoma Cell Line</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2022</publicationYear>
  <dates>
    <date dateType="Issued">2022-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/231626</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1007/s11030-020-10161-8</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">Starting from the 3,5-dimethyl pyrazole ring and acetophenone derivatives, five different N-propargylated C-3 substituted pyrazoles were obtained. These derivatives were reacted with different amine derivatives using Cs2CO3 in methanol and 11 different pyrazolo [1,5-a] pyrazine-4(5H)-one derivatives were obtained, which are not found in the literature. The cytotoxic effects of these derivatives in the A549 cell line were investigated. The 160 mu M concentration of two derivatives was found to increase cell death rate to 50%, and two derivatives increased cell death rate by up to 40%. The structure-activity relationship (SAR) study revealed an amide group with a long alkyl chain and benzene ring with a p-CF3 group could be important for efficiency. With theoretical ADMET studies of pyrazolopyrazine derivatives, pharmacokinetic phases were predicted to be suitable.</description>
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