Diğer Açık Erişim
Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER
<?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.274087</identifier> <creators> <creator> <creatorName>Halilibrahim CIFTCI</creatorName> <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0002-9796-7669</nameIdentifier> <affiliation>Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, Türkiye</affiliation> </creator> <creator> <creatorName>Masami OTSUKA</creatorName> <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0002-2968-3939</nameIdentifier> <affiliation>Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan</affiliation> </creator> <creator> <creatorName>Mikako FUJITA</creatorName> <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0001-6705-4052</nameIdentifier> <affiliation>Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan</affiliation> </creator> <creator> <creatorName>Belgin SEVER</creatorName> <nameIdentifier nameIdentifierScheme="ORCID" schemeURI="http://orcid.org/">0000-0003-4847-9711</nameIdentifier> <affiliation>Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Türkiye</affiliation> </creator> </creators> <titles> <title>Supplementary Information</title> </titles> <publisher>Aperta</publisher> <publicationYear>2024</publicationYear> <subjects> <subject>Naphthalene</subject> <subject>Pyrazoline</subject> <subject>Thiazole</subject> <subject>EGFR</subject> <subject>NSCLC</subject> <subject>Breast cancer</subject> </subjects> <dates> <date dateType="Issued">2024-11-20</date> </dates> <resourceType resourceTypeGeneral="Other"/> <alternateIdentifiers> <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/274087</alternateIdentifier> </alternateIdentifiers> <relatedIdentifiers> <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.48623/aperta.274086</relatedIdentifier> </relatedIdentifiers> <rightsList> <rights rightsURI="https://creativecommons.org/licenses/by-nc/4.0/">Creative Commons Attribution-NonCommercial</rights> <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights> </rightsList> <descriptions> <description descriptionType="Abstract"><p>Epidermal growth factor receptor (EGFR) and HER2, pioneer members of the receptor tyrosine kinase subfamily, are frequently mutated and/or overexpressed in several types of human cancers, including non-small cell lung cancer (NSCLC) and breast cancer, which are leading causes of cancer-related deaths worldwide. &nbsp;EGFR and HER2-focused anti-NSCLC and anti-breast cancer studies encouraged us to search for new potential agents. For this purpose, in the current work, naphthalene-linked pyrazoline-thiazole hybrids (<strong>BTT1-10 </strong>and<strong> BTP1-10) </strong>were synthesized and examined<strong> </strong>for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that <strong>BTT-5</strong> induced strong toxicity in A549 cells with the IC<sub>50</sub> value of 9.51&plusmn;3.35 &mu;M compared to lapatinib (IC<sub>50 </sub>= 16.44&plusmn;3.92 &mu;M). <strong>BTT-5</strong> also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, <strong>BTT-5</strong> augmented apoptosis significantly in A549 cells (18.40%). <strong>BTT-5</strong> displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 &mu;M concentration interpreting its selective kinase inhibitory effects. Molecular docking assessment indicated that <strong>BTT-5</strong> showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, <strong>BTT-5</strong> can serve as a lead for future anti-NSCLC studies.</p></description> </descriptions> </resource>
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