1 Ocak 2020 Dergi makalesi Açık Erişim

Gurdere, Meliha Burcu; Aydin, Ali; Yencilek, Belkiz; Erturk, Fatih; Ozbek, Oguz; Erkan, Sultan; Budak, Yakup; Ceylan, Mustafa

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  "@context": "https://schema.org/", 
  "@id": 4279, 
  "@type": "ScholarlyArticle", 
  "creator": [
    {
      "@type": "Person", 
      "affiliation": "Tokat Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey", 
      "name": "Gurdere, Meliha Burcu"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Yozgat Bozok Univ, Fac Med, Dept Basic Med Sci, TR-66100 Yozgat, Turkey", 
      "name": "Aydin, Ali"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Tokat Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey", 
      "name": "Yencilek, Belkiz"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Istanbul Arel Univ, Vocat Sch, Occupat Hlth & Safety Program, TR-34100 Istanbul, Turkey", 
      "name": "Erturk, Fatih"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Tokat Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey", 
      "name": "Ozbek, Oguz"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Sivas Cumhuriyet Univ, Yildizeli Vocat Sch, Chem & Chem Proc Technol, TR-58140 Sivas, Turkey", 
      "name": "Erkan, Sultan"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Tokat Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey", 
      "name": "Budak, Yakup"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Tokat Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey", 
      "name": "Ceylan, Mustafa"
    }
  ], 
  "datePublished": "2020-01-01", 
  "description": "Novel enamine derivatives were synthesized from the reaction of lactone and chalcones and their antiproliferative and cytotoxic activities against six cancer cell lines (e. g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell lines (e. g., FL) were investigated along with their mode of interactions with CT-DNA. Most of the enamine derivatives with IC(50)values of 86-168 mu M demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5-fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (similar to 6 nm), indicating that they bind to the DNA by way of an intercalative or minor groove binding mode. The binding constants of the compounds are in the range of 0.1x103 M-1-2.3x104 M-1. The antiproliferative activity of studied enamine derivatives could possibly be due to their DNA binding as well as their cytotoxic properties. In addition to these assays, the chalcones and enamine derivatives were investigated by molecular docking to calculate the synergistic effect of antiproliferative activities against six human cancer cell lines.", 
  "headline": "Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives", 
  "identifier": 4279, 
  "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", 
  "license": "http://www.opendefinition.org/licenses/cc-by", 
  "name": "Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives", 
  "url": "https://aperta.ulakbim.gov.tr/record/4279"
}