1 Ocak 2022 Dergi makalesi Açık Erişim

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

Citation Style Language JSON

{
  "DOI": "10.1007/s11030-020-10161-8", 
  "abstract": "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.", 
  "author": [
    {
      "family": "Uygun", 
      "given": " Meltem Tan"
    }, 
    {
      "family": "Amudi", 
      "given": " Karina"
    }, 
    {
      "family": "Turacli", 
      "given": " Irem Dogan"
    }, 
    {
      "family": "Menges", 
      "given": " Nurettin"
    }
  ], 
  "container_title": "MOLECULAR DIVERSITY", 
  "id": "231626", 
  "issue": "1", 
  "issued": {
    "date-parts": [
      [
        2022, 
        1, 
        1
      ]
    ]
  }, 
  "page": "113-124", 
  "title": "A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line", 
  "type": "article-journal", 
  "volume": "26"
}