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dc.contributor.authorKurban, Berkant
dc.contributor.authorSağlık, Begüm Nurpelin
dc.contributor.authorOsmaniye, Derya
dc.contributor.authorLevent, Serkan
dc.contributor.authorÖzkay, Yusuf
dc.contributor.authorKaplancıklı, Zafer Asım
dc.date.accessioned2023-10-12T09:11:55Z
dc.date.available2023-10-12T09:11:55Z
dc.date.issued2023en_US
dc.identifier.citationKurban, B., Sağlık, B. N., Osmaniye, D., Levent, S., Özkay, Y., & Kaplancıklı, Z. A. (2023). Synthesis and Anticancer Activities of Pyrazole–Thiadiazole-Based EGFR Inhibitors. ACS omega, 8(34), 31500-31509.en_US
dc.identifier.issn2470-1343
dc.identifier.urihttps://dx.doi.org/0.1021/acsomega.3c04635.
dc.identifier.urihttps://hdl.handle.net/20.500.12933/1634
dc.description.abstractAbstract Lung cancer is one of the most common cancer types of cancer with the highest mortality rates. However, while epidermal growth factor receptor (EGFR) is an important parameter for lung cancer, EGFR inhibitors also show great promise in the treatment of the disease. Therefore, a series of new EGFR inhibitor candidates containing thiadiazole and pyrazole rings have been developed. The activities of the synthesized compounds were elucidated by in vitro MTT, (which is chemically 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide), cytotoxicity assay, analysis of mitochondrial membrane potential (MMP) by flow cytometry, and EGFR inhibition experiments. Molecular docking and molecular dynamics simulations were performed as in silico studies. Compounds 6d, 6g, and 6j showed inhibitor activity against the A549 cell line with IC50 = 5.176 ± 0.164; 1.537 ± 0.097; and 8.493 ± 0.667 μM values, respectively. As a result of MMP by flow cytometry, compound 6g showed 80.93% mitochondrial membrane potential. According to the results of the obtained EGFR inhibitory assay, compound 6g shows inhibitory activity on the EGFR enzyme with a value of IC50 = 0.024 ± 0.002 μM.en_US
dc.language.isoengen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.isversionof10.1021/acsomega.3c04635.en_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.titleSynthesis and anticancer activities of pyrazole-thiadiazole-based EGFR inhibitorsen_US
dc.typearticleen_US
dc.authorid0000-0002-1595-3870en_US
dc.departmentAFSÜen_US
dc.contributor.institutionauthorKurban, Berkant
dc.identifier.volume8en_US
dc.identifier.issue34en_US
dc.identifier.startpage31500en_US
dc.identifier.endpage31509en_US
dc.relation.journalACS omegaen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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