Dergi makalesi Açık Erişim
Uygun, Meltem Tan; Amudi, Karina; Turacli, Irem Dogan; Menges, Nurettin
<?xml version='1.0' encoding='UTF-8'?> <record xmlns="http://www.loc.gov/MARC21/slim"> <leader>00000nam##2200000uu#4500</leader> <datafield tag="245" ind1=" " ind2=" "> <subfield code="a">A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line</subfield> </datafield> <datafield tag="909" ind1="C" ind2="4"> <subfield code="p">MOLECULAR DIVERSITY</subfield> <subfield code="v">26</subfield> <subfield code="n">1</subfield> <subfield code="c">113-124</subfield> </datafield> <controlfield tag="001">231626</controlfield> <datafield tag="980" ind1=" " ind2=" "> <subfield code="a">user-tubitak-destekli-proje-yayinlari</subfield> </datafield> <datafield tag="520" ind1=" " ind2=" "> <subfield code="a">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.</subfield> </datafield> <datafield tag="650" ind1="1" ind2="7"> <subfield code="2">opendefinition.org</subfield> <subfield code="a">cc-by</subfield> </datafield> <datafield tag="700" ind1=" " ind2=" "> <subfield code="a">Amudi, Karina</subfield> </datafield> <datafield tag="700" ind1=" " ind2=" "> <subfield code="u">Ufuk Univ, Fac Med, Dept Med Biol, TR-06520 Ankara, Turkey</subfield> <subfield code="a">Turacli, Irem Dogan</subfield> </datafield> <datafield tag="700" ind1=" " ind2=" "> <subfield code="a">Menges, Nurettin</subfield> </datafield> <datafield tag="980" ind1=" " ind2=" "> <subfield code="b">article</subfield> <subfield code="a">publication</subfield> </datafield> <datafield tag="542" ind1=" " ind2=" "> <subfield code="l">open</subfield> </datafield> <datafield tag="100" ind1=" " ind2=" "> <subfield code="a">Uygun, Meltem Tan</subfield> </datafield> <datafield tag="260" ind1=" " ind2=" "> <subfield code="c">2022-01-01</subfield> </datafield> <controlfield tag="005">20221007081320.0</controlfield> <datafield tag="909" ind1="C" ind2="O"> <subfield code="o">oai:aperta.ulakbim.gov.tr:231626</subfield> <subfield code="p">user-tubitak-destekli-proje-yayinlari</subfield> </datafield> <datafield tag="856" ind1="4" ind2=" "> <subfield code="z">md5:6f0901a5294cdb5613089060925af50d</subfield> <subfield code="s">236</subfield> <subfield code="u">https://aperta.ulakbim.gov.trrecord/231626/files/bib-084dc618-b862-4674-818a-e7683523cc15.txt</subfield> </datafield> <datafield tag="540" ind1=" " ind2=" "> <subfield code="u">http://www.opendefinition.org/licenses/cc-by</subfield> <subfield code="a">Creative Commons Attribution</subfield> </datafield> <datafield tag="024" ind1=" " ind2=" "> <subfield code="a">10.1007/s11030-020-10161-8</subfield> <subfield code="2">doi</subfield> </datafield> </record>
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