20 Kasım 2024 Diğer Açık Erişim

Halilibrahim ÇİFTÇİ; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

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  <identifier identifierType="DOI">10.48623/aperta.274141</identifier>
  <creators>
    <creator>
      <creatorName>Halilibrahim ÇİFTÇİ</creatorName>
      <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0002-9796-7669</nameIdentifier>
      <affiliation>Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, Türkiye</affiliation>
    </creator>
    <creator>
      <creatorName>Masami OTSUKA</creatorName>
      <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0002-2968-3939</nameIdentifier>
      <affiliation>Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan</affiliation>
    </creator>
    <creator>
      <creatorName>Mikako FUJITA</creatorName>
      <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0001-6705-4052</nameIdentifier>
      <affiliation>Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan</affiliation>
    </creator>
    <creator>
      <creatorName>Belgin SEVER</creatorName>
      <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0003-4847-9711</nameIdentifier>
      <affiliation>Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Türkiye</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Supplementary Information</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2024</publicationYear>
  <subjects>
    <subject>Naphthalene</subject>
    <subject>Pyrazoline</subject>
    <subject>Thiazole</subject>
    <subject>Epidermal growth factor receptor</subject>
    <subject>Nonsmall cell lung cancer</subject>
    <subject>Breast cancer</subject>
  </subjects>
  <dates>
    <date dateType="Issued">2024-11-20</date>
  </dates>
  <resourceType resourceTypeGeneral="Other"/>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/274141</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.48623/aperta.274086</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="https://creativecommons.org/licenses/by-nc/4.0/">Creative Commons Attribution-NonCommercial</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">&lt;p&gt;The epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), pioneer members of the receptor tyrosine kinase subfamily, are frequently mutated and/or overexpressed in several types of human cancers, including nonsmall cell lung cancer (NSCLC) and breast cancer, which are leading causes of cancer-related deaths worldwide. &amp;nbsp;EGFR and HER2-focused anti-NSCLC and antibreast cancer studies encouraged us to search for new potential agents. For this purpose, in the current work, naphthalene-linked pyrazoline-thiazole hybrids (&lt;strong&gt;BTT1-10 &lt;/strong&gt;and&lt;strong&gt; BTP1-10) &lt;/strong&gt;were synthesized and examined&lt;strong&gt; &lt;/strong&gt;for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that &lt;strong&gt;BTT-5&lt;/strong&gt; induced strong toxicity in A549 cells with the IC&lt;sub&gt;50&lt;/sub&gt; value of 9.51&amp;plusmn;3.35 &amp;mu;M compared to lapatinib (IC&lt;sub&gt;50 &lt;/sub&gt;= 16.44&amp;plusmn;3.92 &amp;mu;M). &lt;strong&gt;BTT-5&lt;/strong&gt; also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, &lt;strong&gt;BTT-5&lt;/strong&gt; augmented apoptosis significantly in A549 cells (18.40%). &lt;strong&gt;BTT-5&lt;/strong&gt; displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 &amp;mu;M concentration interpreting its selective kinase inhibitory effects. The molecular docking assessment indicated that &lt;strong&gt;BTT-5&lt;/strong&gt; showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, &lt;strong&gt;BTT-5&lt;/strong&gt; can serve as a lead for future anti-NSCLC studies.&lt;/p&gt;</description>
  </descriptions>
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