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