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Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents

Aktas, Derya Anil; Akinalp, Gokcen; Sanli, Fatma; Yucel, Mehmet Ali; Gambacorta, Nicola; Nicolotti, Orazio; Karatas, Omer Faruk; Algul, Oztekin; Burmaoglu, Serdar


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{
  "DOI": "10.1016/j.bmcl.2020.127427", 
  "abstract": "The present study was carried out in the attempt to synthesize a new class of potential anticancer agents comprising eleven compounds (24-34) sharing the 3,5-diarylisoxazole as a core. The chemical structure of the new synthesized compounds was established by IR, H-1 NMR, C-13 NMR and elemental analysis. Their biological potential towards prostate cancer was evaluated by using cancer PC3 cells and non-tumorigenic PNT1a cells. Interestingly, compound 26 distinguished from others with a quite high selectivity value that is comparable to 5-FU. The binding mode of 26 towards Ribosomal protein S6 kinase beta-1 (S6K1) was investigated at a molecular level of detail by employing docking simulations based on GLIDE standard precision as well as MM-GBSA calculations.", 
  "author": [
    {
      "family": "Aktas", 
      "given": " Derya Anil"
    }, 
    {
      "family": "Akinalp", 
      "given": " Gokcen"
    }, 
    {
      "family": "Sanli", 
      "given": " Fatma"
    }, 
    {
      "family": "Yucel", 
      "given": " Mehmet Ali"
    }, 
    {
      "family": "Gambacorta", 
      "given": " Nicola"
    }, 
    {
      "family": "Nicolotti", 
      "given": " Orazio"
    }, 
    {
      "family": "Karatas", 
      "given": " Omer Faruk"
    }, 
    {
      "family": "Algul", 
      "given": " Oztekin"
    }, 
    {
      "family": "Burmaoglu", 
      "given": " Serdar"
    }
  ], 
  "container_title": "BIOORGANIC & MEDICINAL CHEMISTRY LETTERS", 
  "id": "3571", 
  "issue": "19", 
  "issued": {
    "date-parts": [
      [
        2020, 
        1, 
        1
      ]
    ]
  }, 
  "title": "Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents", 
  "type": "article-journal", 
  "volume": "30"
}
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