Diğer Açık Erişim
Halilibrahim CIFTCI; Masami OTSUKA; Mikako FUJITA; Belgin SEVER
{ "@context": "https://schema.org/", "@id": 274087, "@type": "CreativeWork", "creator": [ { "@id": "https://orcid.org/0000-0002-9796-7669", "@type": "Person", "affiliation": "Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, T\u00fcrkiye", "name": "Halilibrahim CIFTCI" }, { "@id": "https://orcid.org/0000-0002-2968-3939", "@type": "Person", "affiliation": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan", "name": "Masami OTSUKA" }, { "@id": "https://orcid.org/0000-0001-6705-4052", "@type": "Person", "affiliation": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan", "name": "Mikako FUJITA" }, { "@id": "https://orcid.org/0000-0003-4847-9711", "@type": "Person", "affiliation": "Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, T\u00fcrkiye", "name": "Belgin SEVER" } ], "datePublished": "2024-11-20", "description": "<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. 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±3.35 μM compared to lapatinib (IC<sub>50 </sub>= 16.44±3.92 μM). <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 μM 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>", "identifier": 274087, "keywords": [ "Naphthalene", "Pyrazoline", "Thiazole", "EGFR", "NSCLC", "Breast cancer" ], "license": "https://creativecommons.org/licenses/by-nc/4.0/", "name": "Supplementary Information", "url": "https://aperta.ulakbim.gov.tr/record/274087" }
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