20 Kasım 2024 Diğer Açık Erişim

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

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{
  "@context": "https://schema.org/", 
  "@id": 274116, 
  "@type": "CreativeWork", 
  "creator": [
    {
      "@id": "https://orcid.org/0000-0002-9796-7669", 
      "@type": "Person", 
      "affiliation": "Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, T\u00fcrkiye", 
      "name": "Halilibrahim CIFTCI"
    }, 
    {
      "@id": "https://orcid.org/0000-0002-2968-3939", 
      "@type": "Person", 
      "affiliation": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan", 
      "name": "Masami OTSUKA"
    }, 
    {
      "@id": "https://orcid.org/0000-0001-6705-4052", 
      "@type": "Person", 
      "affiliation": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan", 
      "name": "Mikako FUJITA"
    }, 
    {
      "@id": "https://orcid.org/0000-0003-4847-9711", 
      "@type": "Person", 
      "affiliation": "Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, T\u00fcrkiye", 
      "name": "Belgin SEVER"
    }
  ], 
  "datePublished": "2024-11-20", 
  "description": "<p>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. &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 (<strong>BTT1-10 </strong>and<strong> BTP1-10) </strong>were synthesized and examined<strong> </strong>for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that <strong>BTT-5</strong> induced strong toxicity in A549 cells with the IC<sub>50</sub> value of 9.51&plusmn;3.35 &mu;M compared to lapatinib (IC<sub>50 </sub>= 16.44&plusmn;3.92 &mu;M). <strong>BTT-5</strong> also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, <strong>BTT-5</strong> augmented apoptosis significantly in A549 cells (18.40%). <strong>BTT-5</strong> displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 &mu;M concentration interpreting its selective kinase inhibitory effects. Molecular docking assessment indicated that <strong>BTT-5</strong> showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, <strong>BTT-5</strong> can serve as a lead for future anti-NSCLC studies.</p>", 
  "identifier": 274116, 
  "keywords": [
    "Naphthalene", 
    "Pyrazoline", 
    "Thiazole", 
    "EGFR", 
    "NSCLC", 
    "Breast cancer"
  ], 
  "license": "https://creativecommons.org/licenses/by-nc/4.0/", 
  "name": "Supplementary Information", 
  "url": "https://aperta.ulakbim.gov.tr/record/274116"
}