Dergi makalesi Açık Erişim
ARZUK Ege; KARAKUŞ Fuat; ERGÜÇ Ali; KUZU Burak
<?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">Novel Pyrazole Derivatives Bearing Carbonitrile and Substituted Thiazole Moiety for Selective COX-2 Inhibition</subfield> </datafield> <datafield tag="024" ind1=" " ind2=" "> <subfield code="a">10.48623/aperta.273717</subfield> <subfield code="2">doi</subfield> </datafield> <controlfield tag="001">273717</controlfield> <datafield tag="520" ind1=" " ind2=" "> <subfield code="a"><p>In this study, a series of derivatives of pyrazole hybrid structurescontaining carbonitrile and substituted thiazole moiety weredesigned to search for selective COX-2 inhibition. The designedtarget structures were synthesized with easy, practical, andefficient procedures. COX-1/2 inhibition and cytotoxic effects ofthe synthesized compounds were evaluated in NIH/3T3 andMDA-MD-231 cell lines for inhibition concentration and selectiv-ity index. The results showed that the compounds have aninhibitory effect with higher selectivity towards COX-2 overall inboth cell lines and moderate antiproliferative activity bytargeting the breast cancer cell line MDA-MB-231. Among the19 compounds synthesized (19 a&ndash;t), especially compound 19 mwas found to be highly effective with COX-2 inhibition of5.63 &mu;M in the NIH/3T3 cell line and 4.12 &mu;M in the MDA-MB-231 cell line. Moreover, molecular docking studies showed thatthe compounds indeed exhibited higher affinity for the COX-2active site. The theoretical ADMET properties of the presentedcompounds were calculated, and the results showed that thecompounds may have a more favorable pharmacokinetic effectprofile than the selective COX-2 inhibitor Celecoxib, thuspromising COX-2 inhibitor drug candidates for the future.</p></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="u">Van YYU</subfield> <subfield code="a">KARAKUŞ Fuat</subfield> </datafield> <datafield tag="700" ind1=" " ind2=" "> <subfield code="u">İzmir Katip Çelebi</subfield> <subfield code="a">ERGÜÇ Ali</subfield> </datafield> <datafield tag="700" ind1=" " ind2=" "> <subfield code="a">KUZU Burak</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="u">Ege Uni</subfield> <subfield code="a">ARZUK Ege</subfield> </datafield> <datafield tag="260" ind1=" " ind2=" "> <subfield code="c">2024-01-02</subfield> </datafield> <controlfield tag="005">20240701062746.0</controlfield> <datafield tag="773" ind1=" " ind2=" "> <subfield code="n">doi</subfield> <subfield code="a">10.48623/aperta.273716</subfield> <subfield code="i">isVersionOf</subfield> </datafield> <datafield tag="909" ind1="C" ind2="O"> <subfield code="o">oai:aperta.ulakbim.gov.tr:273717</subfield> </datafield> <datafield tag="856" ind1="4" ind2=" "> <subfield code="z">md5:edfcbcdf8656b79c219a4dfb3704752d</subfield> <subfield code="s">6657728</subfield> <subfield code="u">https://aperta.ulakbim.gov.trrecord/273717/files/ChemistrySelect - 2024 - kuzu.pdf</subfield> </datafield> <datafield tag="540" ind1=" " ind2=" "> <subfield code="u">http://www.opendefinition.org/licenses/cc-by-sa</subfield> <subfield code="a">Creative Commons Attribution Share-Alike</subfield> </datafield> </record>
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