20 Kasım 2024 Diğer Açık Erişim

Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER

JSON

{
  "conceptdoi": "10.48623/aperta.274086", 
  "conceptrecid": "274086", 
  "created": "2024-11-20T12:49:30.538494+00:00", 
  "doi": "10.48623/aperta.274087", 
  "files": [
    {
      "bucket": "d87b8d7e-7556-48e9-97dc-4c9a13b63dbc", 
      "checksum": "md5:d47702671bf43bd07ed0bbff0b55ecb8", 
      "key": "Supplementary Information.pdf", 
      "links": {
        "self": "https://aperta.ulakbim.gov.tr/api/files/d87b8d7e-7556-48e9-97dc-4c9a13b63dbc/Supplementary%20Information.pdf"
      }, 
      "size": 6601423, 
      "type": "pdf"
    }
  ], 
  "id": 274087, 
  "links": {
    "badge": "https://aperta.ulakbim.gov.tr/badge/doi/10.48623/aperta.274087.svg", 
    "bucket": "https://aperta.ulakbim.gov.tr/api/files/d87b8d7e-7556-48e9-97dc-4c9a13b63dbc", 
    "conceptbadge": "https://aperta.ulakbim.gov.tr/badge/doi/10.48623/aperta.274086.svg", 
    "conceptdoi": "https://doi.org/10.48623/aperta.274086", 
    "doi": "https://doi.org/10.48623/aperta.274087", 
    "html": "https://aperta.ulakbim.gov.tr/record/274087", 
    "latest": "https://aperta.ulakbim.gov.tr/api/records/274141", 
    "latest_html": "https://aperta.ulakbim.gov.tr/record/274141"
  }, 
  "metadata": {
    "access_right": "open", 
    "access_right_category": "success", 
    "creators": [
      {
        "affiliation": "Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, T\u00fcrkiye", 
        "name": "Halilibrahim CIFTCI", 
        "orcid": "0000-0002-9796-7669"
      }, 
      {
        "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"
      }, 
      {
        "affiliation": "Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, T\u00fcrkiye", 
        "name": "Belgin SEVER", 
        "orcid": "0000-0003-4847-9711"
      }
    ], 
    "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>", 
    "doi": "10.48623/aperta.274087", 
    "has_grant": false, 
    "keywords": [
      "Naphthalene", 
      "Pyrazoline", 
      "Thiazole", 
      "EGFR", 
      "NSCLC", 
      "Breast cancer"
    ], 
    "license": {
      "id": "cc-by-nc-4.0"
    }, 
    "publication_date": "2024-11-20", 
    "related_identifiers": [
      {
        "identifier": "10.48623/aperta.274086", 
        "relation": "isVersionOf", 
        "scheme": "doi"
      }
    ], 
    "relations": {
      "version": [
        {
          "count": 3, 
          "index": 0, 
          "is_last": false, 
          "last_child": {
            "pid_type": "recid", 
            "pid_value": "274141"
          }, 
          "parent": {
            "pid_type": "recid", 
            "pid_value": "274086"
          }
        }
      ]
    }, 
    "resource_type": {
      "title": "Di\u011fer", 
      "type": "other"
    }, 
    "science_branches": [
      "Sa\u011fl\u0131k Bilimleri > Eczac\u0131l\u0131k > Meslek Bilimleri > Farmas\u00f6tik Kimya"
    ], 
    "title": "Supplementary Information"
  }, 
  "owners": [
    2512
  ], 
  "revision": 3, 
  "stats": {
    "downloads": 45.0, 
    "unique_downloads": 40.0, 
    "unique_views": 100.0, 
    "version_downloads": 145.0, 
    "version_unique_downloads": 125.0, 
    "version_unique_views": 793.0, 
    "version_views": 1146.0, 
    "version_volume": 964224145.0, 
    "views": 124.0, 
    "volume": 297064035.0
  }, 
  "updated": "2024-12-18T07:44:50.209765+00:00"
}