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A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line

Uygun, Meltem Tan; Amudi, Karina; Turacli, Irem Dogan; Menges, Nurettin


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{
  "@context": "https://schema.org/", 
  "@id": 231626, 
  "@type": "ScholarlyArticle", 
  "creator": [
    {
      "@type": "Person", 
      "name": "Uygun, Meltem Tan"
    }, 
    {
      "@type": "Person", 
      "name": "Amudi, Karina"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Ufuk Univ, Fac Med, Dept Med Biol, TR-06520 Ankara, Turkey", 
      "name": "Turacli, Irem Dogan"
    }, 
    {
      "@type": "Person", 
      "name": "Menges, Nurettin"
    }
  ], 
  "datePublished": "2022-01-01", 
  "description": "Starting from the 3,5-dimethyl pyrazole ring and acetophenone derivatives, five different N-propargylated C-3 substituted pyrazoles were obtained. These derivatives were reacted with different amine derivatives using Cs2CO3 in methanol and 11 different pyrazolo [1,5-a] pyrazine-4(5H)-one derivatives were obtained, which are not found in the literature. The cytotoxic effects of these derivatives in the A549 cell line were investigated. The 160 mu M concentration of two derivatives was found to increase cell death rate to 50%, and two derivatives increased cell death rate by up to 40%. The structure-activity relationship (SAR) study revealed an amide group with a long alkyl chain and benzene ring with a p-CF3 group could be important for efficiency. With theoretical ADMET studies of pyrazolopyrazine derivatives, pharmacokinetic phases were predicted to be suitable.", 
  "headline": "A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line", 
  "identifier": 231626, 
  "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", 
  "license": "http://www.opendefinition.org/licenses/cc-by", 
  "name": "A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line", 
  "url": "https://aperta.ulakbim.gov.tr/record/231626"
}
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