Design, synthesis and molecular modeling studies of thiosemicarbazide & thiazolyl-hydrazone derivatives as potential anticancer agents and topoisomerase inhibitors

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dc.authoridCevik, Ozge/0000-0002-9325-3757
dc.authorwosidYilmaz Ozguven, Serap/G-1553-2014
dc.authorwosidCevik, Ozge/F-1326-2014
dc.contributor.authorSenkardes, Sevil
dc.contributor.authorBolat, Irfan
dc.contributor.authorSahinbey, Hazal
dc.contributor.authorKarakus, Sevgi
dc.contributor.authorErdogan, Omer
dc.contributor.authorCanturk, Pakize
dc.contributor.authorOzguven, Serap Yilmaz
dc.date.accessioned2024-06-12T11:16:16Z
dc.date.available2024-06-12T11:16:16Z
dc.date.issued2024
dc.departmentTrakya Üniversitesien_US
dc.description.abstractThis study involved the design, synthesis and evaluation of a series of novel thiosemicarbazide and thiazolylhydrazone derivatives. The synthesized compounds were tested for cytotoxic effects SH-SY5Y neuroblastoma cells, as well as NIH-3T3 normal cell line using the MTT assay. Among the tested compounds, 3b, 3d, 3i, 4b, 4d and 4i exhibited IC50 values ranging from 1.97 mu M to 3.22 mu M in the SH-SY5Y cancer cell line with lower cytotoxicity toward NIH-3T3 cells. Moreover, all compounds were also screened for their topoisomerase I and II inhibitory activity and compound 3b completely inhibited the topoisomerase I enzyme, whereas all compounds showed potent topoisomerase II inhibitory activity. Docking studies were performed to identify the mode of binding of the tested compounds to the active site of topoisomerase I and II. In conclusion, N-(4-(2-((2-chlor- ophenyl)carbamothioyl)hydrazine-1-carbonyl)phenyl)benzamide (3b) emerges as a promising inhibitor of topoisomerase I and II and holds potential as a lead compound in the quest for novel anticancer agents.en_US
dc.description.sponsorshipTUBITAK 2209-A Research Projects Program [1919B012100684]en_US
dc.description.sponsorshipThis work was supported by a TUBITAK 2209-A Research Projects Program. (No: 1919B012100684) .en_US
dc.identifier.doi10.1016/j.molstruc.2024.137488
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85181941521en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2024.137488
dc.identifier.urihttps://hdl.handle.net/20.500.14551/24258
dc.identifier.volume1302en_US
dc.identifier.wosWOS:001158311700001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofJournal Of Molecular Structureen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectThiosemicarbazideen_US
dc.subjectThiazoleen_US
dc.subjectAnticanceren_US
dc.subjectTopoisomeraseen_US
dc.subjectDocking Studyen_US
dc.subjectBiological Evaluationen_US
dc.subjectTargetsen_US
dc.subjectStranden_US
dc.titleDesign, synthesis and molecular modeling studies of thiosemicarbazide & thiazolyl-hydrazone derivatives as potential anticancer agents and topoisomerase inhibitorsen_US
dc.typeArticleen_US

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