20 Kasım 2024 Diğer Açık Erişim

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

Citation Style Language JSON

{
  "URL": "https://aperta.ulakbim.gov.tr/record/274087", 
  "abstract": "<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>", 
  "author": [
    {
      "family": "Halilibrahim CIFTCI"
    }, 
    {
      "family": "Masami OTSUKA"
    }, 
    {
      "family": "Mikako FUJITA"
    }, 
    {
      "family": "Belgin SEVER"
    }
  ], 
  "id": "274087", 
  "issued": {
    "date-parts": [
      [
        2024, 
        11, 
        20
      ]
    ]
  }, 
  "title": "Supplementary Information", 
  "type": "article"
}