Synthesis and molecular modeling of metap2 of thiosemicarbazides, 1,2,4-triazoles, thioethers derived from (S)-naproxen as possible breast cancer agents

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dc.contributor.authorA. I., Uba
dc.contributor.authorO., Çuhadar
dc.contributor.authorS.K., Sevinç
dc.contributor.authorS., Tiryaki
dc.contributor.authorP. M., Timer
dc.contributor.authorO., Orun
dc.contributor.authorTelçi, D.
dc.contributor.authorYılmaz, Ö.
dc.contributor.authorYelekçi, K.
dc.contributor.authorKüçükgüzel, Güniz
dc.date.accessioned2022-03-22T11:30:35Z
dc.date.available2022-03-22T11:30:35Z
dc.date.issued2022en_US
dc.departmentFakülteler, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalıen_US
dc.description.abstractNew thiosemicarbazides (3, 5-6), 1,2,4-triazoles (14-15) and thioethers (22-68) from derived (S)-Naproxen were synthesized in this study. The structure of these compounds were elucidated by spectral (FT-IR, 1H NMR, 13C NMR) methods, besides elemental analysis and TLC. The molecular binding of the compounds on MetAP-2 was performed. Anticancer effects of the synthesized compounds were studied by using MTT assay method on MCF-7 (includes oestrogene and progesterone receptors) and MDA-MB-231 (lacks estrogen and progesterone receptors) adenocarcinoma cell lines at 0, 10, 25, 50, 75 and 100 μM concentrations for 24 h. The IC50 values of novel (S)-Naproxen derivatives were determined between from 5 to 100 μM on MCF-7 breast cancer cell line and MDA-MB-231 cell lines. The apoptotic activity of selected compounds 22 and 42 were first analyzed by Annexin V staining using Tali Image-Based Cytometer. Mitochondrial membrane potential changes determined in fluorescence plate reader following JC-1 stain for compounds 22 and 42 in MCF-7 and MDA-MB-231 cells. The effect of these compounds on the cell viability 4T1 mouse mammary tumor cell line was tested at 1 to 5 times of calculated IC50 value (IC50x1, IC50x2, IC50x3, IC50x4, and IC50x5). Next in order to determine the toxicity of the combination of compound 51 and Docetaxel, WST-1 cell viability and proliferation assay was performed with 4T1.en_US
dc.identifier.citationBirgül, K., Uba, A. I., Çuhadar, O., Sevinç, S. K., Tiryaki, S., Tiber, P. M., ... & Küçükgüzel, Ş. G. (2022). Synthesis and Molecular Modeling of MetAP2 of Thiosemicarbazides, 1, 2, 4-triazoles, thioethers derived from (S)-Naproxen as Possible Breast Cancer Agents. Journal of Molecular Structure.en_US
dc.identifier.issn0022-2860
dc.identifier.scopus2-s2.0-85125952901
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://hdl.handle.net/20.500.12939/2300
dc.identifier.volume1259en_US
dc.identifier.wosWOS:000820364800009
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorK., Birgül
dc.language.isoen
dc.publisherJournal of Molecular Structureen_US
dc.relation.ispartofJournal of Molecular Structure
dc.relation.isversionof10.1016/j.molstruc.2022.132739en_US
dc.relation.publicationcategoryMakale - Ulusal Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectApoptosisen_US
dc.subjectBreast Cancer Cell Lineen_US
dc.subjectMetAP2en_US
dc.subjectNaproxenen_US
dc.subjectThioetheren_US
dc.subjectTriple Negative Canceren_US
dc.titleSynthesis and molecular modeling of metap2 of thiosemicarbazides, 1,2,4-triazoles, thioethers derived from (S)-naproxen as possible breast cancer agents
dc.typeArticle

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