Design, Synthesis and Anticancer Activity Studies of Novel 4-Butylaminophenyl Hydrazide-Hydrazones as Apoptotic Inducers

dc.contributor.author Küçükgüzel, Şükriye Güniz
dc.contributor.author Baysal, Ozge Deniz Yesil
dc.contributor.author Basaran, Guzide Satir
dc.contributor.author Sezer, Gulay
dc.contributor.author Telci, Dilek
dc.contributor.author Kucukguzel, S. Guniz
dc.contributor.other Eczacılık Meslek Bilimleri Bölümü
dc.date.accessioned 2025-01-11T13:01:01Z
dc.date.available 2025-01-11T13:01:01Z
dc.date.issued 2022
dc.description Han, Muhammed Ihsan/0000-0001-5610-0869 en_US
dc.description.abstract In this study, a series of the novel Tetracaine derivatives bearing hydrazide-hydrazone moiety were designed, synthesized, and evaluated for anticancer activity. The structures of these compounds were characterized by spectral (H-1-C-13 NMR, FT-IR, and HR-MS analyses) methods. All synthesized compounds (2a-1) were screened for anticancer activity against human hepatocellular carcinoma (HepG2) and lung carcinoma (A549) cell lines. Against HepG2 and A549 cell lines, among the synthesized compounds, 4-(Butylamino)-N'-[(2,4-dichlorophenyl)methylidene]benzohydrazide (2i) demonstrated the most potent anticancer activity with IC50 values 28 and 7 mu M, respectively. Possible cytotoxic effects of compounds (2a-1) on both normal human lung fibroblast (MCR-5) and normal human dermal fibroblast (HDF) cell lines were assessed. Inhibition of anti-apoptotic protein Bax and Bcl-2 was investigated in HepG2 and A549 cells treated with compound 2i using qRT-PCR. Apoptosis was also detected by Annexin V studies. The flow cytometric analysis results showed that compound 2i treatment of HepG2 and A549 cells significantly increased apoptotic cell populations while decreasing viabilities in these carcinomas in a dose-dependent manner after 72 h of incubation. (C) 2022 Elsevier Ltd. All rights reserved. en_US
dc.identifier.citation 13
dc.identifier.doi 10.1016/j.tet.2022.132797
dc.identifier.issn 0040-4020
dc.identifier.issn 1464-5416
dc.identifier.scopus 2-s2.0-85130334037
dc.identifier.uri https://doi.org/10.1016/j.tet.2022.132797
dc.identifier.uri https://hdl.handle.net/20.500.14627/94
dc.language.iso en en_US
dc.publisher Pergamon-elsevier Science Ltd en_US
dc.rights info:eu-repo/semantics/closedAccess en_US
dc.subject Tetracaine en_US
dc.subject Hydrazide-Hydrazone en_US
dc.subject Anticancer Activity en_US
dc.subject Qrt-Pcr en_US
dc.subject Annexin V en_US
dc.title Design, Synthesis and Anticancer Activity Studies of Novel 4-Butylaminophenyl Hydrazide-Hydrazones as Apoptotic Inducers en_US
dc.type Article en_US
dspace.entity.type Publication
gdc.author.id Han, Muhammed Ihsan/0000-0001-5610-0869
gdc.author.scopusid 57196050609
gdc.author.scopusid 57700917900
gdc.author.scopusid 57218109937
gdc.author.scopusid 25927611300
gdc.author.scopusid 24766838100
gdc.author.scopusid 55894906300
gdc.author.wosid HAN, MUHAMMED İHSAN/ADF-1623-2022
gdc.author.wosid Telci, Dilek/N-5053-2019
gdc.author.wosid Küçükgüzel, Ş.Güniz/AAQ-8954-2021
gdc.description.department Fenerbahçe University en_US
gdc.description.departmenttemp [Han, M. Ihsan] Erciyes Univ, Fac Pharm, Dept Pharmaceut Chem, TR-38039 Kayseri, Turkey; [Baysal, Ozge Deniz Yesil; Telci, Dilek] Yeditepe Univ, Fac Engn, Dept Genet & Bioengn, TR-34755 Istanbul, Turkey; [Basaran, Guzide Satir] Erciyes Univ, Fac Pharm, Dept Pharmaceut Biochem, TR-38039 Kayseri, Turkey; [Basaran, Guzide Satir; Sezer, Gulay] Erciyes Univ, Genom & Stem Cell Ctr, TR-38039 Kayseri, Turkey; [Sezer, Gulay] Erciyes Univ, Fac Med, Dept Pharmacol, TR-38039 Kayseri, Turkey; [Kucukguzel, S. Guniz] Fenerbahce Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34758 Istanbul, Turkey en_US
gdc.description.publicationcategory Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı en_US
gdc.description.scopusquality Q3
gdc.description.volume 115 en_US
gdc.description.woscitationindex Science Citation Index Expanded - Index Chemicus
gdc.description.wosquality Q3
gdc.identifier.wos WOS:000832692800007
gdc.scopus.citedcount 18
gdc.wos.citedcount 16
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