20 Kasım 2024 Diğer Açık Erişim

Halilibrahim ÇİFTÇİ; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

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      {
        "affiliation": "Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, T\u00fcrkiye", 
        "name": "Halilibrahim \u00c7\u0130FT\u00c7\u0130", 
        "orcid": "0000-0002-9796-7669"
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      {
        "affiliation": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan", 
        "name": "Masami OTSUKA", 
        "orcid": "0000-0002-2968-3939"
      }, 
      {
        "affiliation": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan", 
        "name": "Mikako FUJITA", 
        "orcid": "0000-0001-6705-4052"
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      {
        "affiliation": "Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, T\u00fcrkiye", 
        "name": "Belgin SEVER", 
        "orcid": "0000-0003-4847-9711"
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    "description": "<p>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. &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 (<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. The 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>", 
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    "keywords": [
      "Naphthalene", 
      "Pyrazoline", 
      "Thiazole", 
      "Epidermal growth factor receptor", 
      "Nonsmall cell lung cancer", 
      "Breast cancer"
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    "publication_date": "2024-11-20", 
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    "science_branches": [
      "Sa\u011fl\u0131k Bilimleri > Eczac\u0131l\u0131k > Meslek Bilimleri > Farmas\u00f6tik Kimya"
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    "title": "Supplementary Information"
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