20 Kasım 2024 Diğer Açık Erişim

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

MARC21 XML

<?xml version='1.0' encoding='UTF-8'?>
<record xmlns="http://www.loc.gov/MARC21/slim">
  <leader>00000nam##2200000uu#4500</leader>
  <datafield tag="245" ind1=" " ind2=" ">
    <subfield code="a">Supplementary Information</subfield>
  </datafield>
  <datafield tag="024" ind1=" " ind2=" ">
    <subfield code="a">10.48623/aperta.274087</subfield>
    <subfield code="2">doi</subfield>
  </datafield>
  <controlfield tag="001">274087</controlfield>
  <datafield tag="520" ind1=" " ind2=" ">
    <subfield code="a">&lt;p&gt;Epidermal growth factor receptor (EGFR) and HER2, pioneer members of the receptor tyrosine kinase subfamily, are frequently mutated and/or overexpressed in several types of human cancers, including non-small 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 anti-breast 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. 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;</subfield>
  </datafield>
  <datafield tag="650" ind1="1" ind2="7">
    <subfield code="2">opendefinition.org</subfield>
    <subfield code="a">cc-by</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="0">(orcid)0000-0002-2968-3939</subfield>
    <subfield code="u">Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan</subfield>
    <subfield code="a">Masami OTSUKA</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="0">(orcid)0000-0001-6705-4052</subfield>
    <subfield code="u">Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan</subfield>
    <subfield code="a">Mikako FUJITA</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="0">(orcid)0000-0003-4847-9711</subfield>
    <subfield code="u">Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Türkiye</subfield>
    <subfield code="a">Belgin SEVER</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">other</subfield>
  </datafield>
  <datafield tag="542" ind1=" " ind2=" ">
    <subfield code="l">open</subfield>
  </datafield>
  <datafield tag="100" ind1=" " ind2=" ">
    <subfield code="0">(orcid)0000-0002-9796-7669</subfield>
    <subfield code="u">Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, Türkiye</subfield>
    <subfield code="a">Halilibrahim CIFTCI</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">Naphthalene</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">Pyrazoline</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">Thiazole</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">EGFR</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">NSCLC</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">Breast cancer</subfield>
  </datafield>
  <datafield tag="260" ind1=" " ind2=" ">
    <subfield code="c">2024-11-20</subfield>
  </datafield>
  <controlfield tag="005">20241120124930.0</controlfield>
  <datafield tag="773" ind1=" " ind2=" ">
    <subfield code="n">doi</subfield>
    <subfield code="a">10.48623/aperta.274086</subfield>
    <subfield code="i">isVersionOf</subfield>
  </datafield>
  <datafield tag="909" ind1="C" ind2="O">
    <subfield code="o">oai:aperta.ulakbim.gov.tr:274087</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="z">md5:d47702671bf43bd07ed0bbff0b55ecb8</subfield>
    <subfield code="s">6601423</subfield>
    <subfield code="u">https://aperta.ulakbim.gov.trrecord/274087/files/Supplementary Information.pdf</subfield>
  </datafield>
  <datafield tag="540" ind1=" " ind2=" ">
    <subfield code="u">https://creativecommons.org/licenses/by-nc/4.0/</subfield>
    <subfield code="a">Creative Commons Attribution-NonCommercial</subfield>
  </datafield>
</record>