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Novel Pyrazole Derivatives Bearing Carbonitrile and Substituted Thiazole Moiety for Selective COX-2 Inhibition

ARZUK Ege; KARAKUŞ Fuat; ERGÜÇ Ali; KUZU Burak


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  <identifier identifierType="DOI">10.48623/aperta.273717</identifier>
  <creators>
    <creator>
      <creatorName>ARZUK Ege</creatorName>
      <affiliation>Ege Uni</affiliation>
    </creator>
    <creator>
      <creatorName>KARAKUŞ Fuat</creatorName>
      <affiliation>Van YYU</affiliation>
    </creator>
    <creator>
      <creatorName>ERGÜÇ Ali</creatorName>
      <affiliation>İzmir Katip Çelebi</affiliation>
    </creator>
    <creator>
      <creatorName>KUZU Burak</creatorName>
    </creator>
  </creators>
  <titles>
    <title>Novel Pyrazole Derivatives Bearing Carbonitrile And Substituted Thiazole Moiety For Selective Cox-2 Inhibition</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2024</publicationYear>
  <dates>
    <date dateType="Issued">2024-01-02</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/273717</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.48623/aperta.273716</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://www.opendefinition.org/licenses/cc-by-sa">Creative Commons Attribution Share-Alike</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">&lt;p&gt;In this study, a series of derivatives of pyrazole hybrid structurescontaining carbonitrile and substituted thiazole moiety weredesigned to search for selective COX-2 inhibition. The designedtarget structures were synthesized with easy, practical, andefficient procedures. COX-1/2 inhibition and cytotoxic effects ofthe synthesized compounds were evaluated in NIH/3T3 andMDA-MD-231 cell lines for inhibition concentration and selectiv-ity index. The results showed that the compounds have aninhibitory effect with higher selectivity towards COX-2 overall inboth cell lines and moderate antiproliferative activity bytargeting the breast cancer cell line MDA-MB-231. Among the19 compounds synthesized (19 a&amp;ndash;t), especially compound 19 mwas found to be highly effective with COX-2 inhibition of5.63 &amp;mu;M in the NIH/3T3 cell line and 4.12 &amp;mu;M in the MDA-MB-231 cell line. Moreover, molecular docking studies showed thatthe compounds indeed exhibited higher affinity for the COX-2active site. The theoretical ADMET properties of the presentedcompounds were calculated, and the results showed that thecompounds may have a more favorable pharmacokinetic effectprofile than the selective COX-2 inhibitor Celecoxib, thuspromising COX-2 inhibitor drug candidates for the future.&lt;/p&gt;</description>
  </descriptions>
  <fundingReferences>
    <fundingReference>
      <funderName>Türkiye Bilimsel ve Teknolojik Araştirma Kurumu</funderName>
      <funderIdentifier funderIdentifierType="Crossref Funder ID">https://doi.org/10.13039/501100004410</funderIdentifier>
      <awardNumber>223S065</awardNumber>
    </fundingReference>
  </fundingReferences>
</resource>
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