20 Kasım 2024 Diğer Açık Erişim

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

Dublin Core

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<oai_dc:dc xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xsi:schemaLocation="http://www.openarchives.org/OAI/2.0/oai_dc/ http://www.openarchives.org/OAI/2.0/oai_dc.xsd">
  <dc:creator>Halilibrahim CIFTCI</dc:creator>
  <dc:creator>Masami OTSUKA</dc:creator>
  <dc:creator>Mikako FUJITA</dc:creator>
  <dc:creator>Belgin SEVER</dc:creator>
  <dc:date>2024-11-20</dc:date>
  <dc:description>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.  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 (BTT1-10 and BTP1-10) were synthesized and examined for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that BTT-5 induced strong toxicity in A549 cells with the IC50 value of 9.51±3.35 μM compared to lapatinib (IC50 = 16.44±3.92 μM). BTT-5 also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, BTT-5 augmented apoptosis significantly in A549 cells (18.40%). BTT-5 displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 μM concentration interpreting its selective kinase inhibitory effects. Molecular docking assessment indicated that BTT-5 showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, BTT-5 can serve as a lead for future anti-NSCLC studies.</dc:description>
  <dc:identifier>https://aperta.ulakbim.gov.trrecord/274116</dc:identifier>
  <dc:identifier>oai:aperta.ulakbim.gov.tr:274116</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>https://creativecommons.org/licenses/by-nc/4.0/</dc:rights>
  <dc:subject>Naphthalene</dc:subject>
  <dc:subject>Pyrazoline</dc:subject>
  <dc:subject>Thiazole</dc:subject>
  <dc:subject>EGFR</dc:subject>
  <dc:subject>NSCLC</dc:subject>
  <dc:subject>Breast cancer</dc:subject>
  <dc:title>Supplementary Information</dc:title>
  <dc:type>info:eu-repo/semantics/other</dc:type>
  <dc:type>other</dc:type>
</oai_dc:dc>