Dergi makalesi Açık Erişim
ARZUK Ege; KARAKUŞ Fuat; ERGÜÇ Ali; KUZU Burak
<?xml version='1.0' encoding='utf-8'?> <resource xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xmlns="http://datacite.org/schema/kernel-4" xsi:schemaLocation="http://datacite.org/schema/kernel-4 http://schema.datacite.org/meta/kernel-4.1/metadata.xsd"> <identifier identifierType="DOI">10.48623/aperta.273717</identifier> <creators> <creator> <creatorName>ARZUK Ege</creatorName> <affiliation>Ege Uni</affiliation> </creator> <creator> <creatorName>KARAKUŞ Fuat</creatorName> <affiliation>Van YYU</affiliation> </creator> <creator> <creatorName>ERGÜÇ Ali</creatorName> <affiliation>İzmir Katip Çelebi</affiliation> </creator> <creator> <creatorName>KUZU Burak</creatorName> </creator> </creators> <titles> <title>Novel Pyrazole Derivatives Bearing Carbonitrile And Substituted Thiazole Moiety For Selective Cox-2 Inhibition</title> </titles> <publisher>Aperta</publisher> <publicationYear>2024</publicationYear> <dates> <date dateType="Issued">2024-01-02</date> </dates> <resourceType resourceTypeGeneral="Text">Journal article</resourceType> <alternateIdentifiers> <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/273717</alternateIdentifier> </alternateIdentifiers> <relatedIdentifiers> <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.48623/aperta.273716</relatedIdentifier> </relatedIdentifiers> <rightsList> <rights rightsURI="http://www.opendefinition.org/licenses/cc-by-sa">Creative Commons Attribution Share-Alike</rights> <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights> </rightsList> <descriptions> <description descriptionType="Abstract"><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></description> </descriptions> <fundingReferences> <fundingReference> <funderName>Türkiye Bilimsel ve Teknolojik Araştirma Kurumu</funderName> <funderIdentifier funderIdentifierType="Crossref Funder ID">https://doi.org/10.13039/501100004410</funderIdentifier> <awardNumber>223S065</awardNumber> </fundingReference> </fundingReferences> </resource>
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Görüntülenme | 64 | 64 |
İndirme | 18 | 18 |
Veri hacmi | 119.8 MB | 119.8 MB |
Tekil görüntülenme | 61 | 61 |
Tekil indirme | 16 | 16 |