Senkardes, SevilBolat, IrfanSahinbey, HazalKarakus, SevgiErdogan, OmerCanturk, PakizeOzguven, Serap Yilmaz2024-06-122024-06-1220240022-28601872-8014https://doi.org/10.1016/j.molstruc.2024.137488https://hdl.handle.net/20.500.14551/24258This 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.en10.1016/j.molstruc.2024.137488info:eu-repo/semantics/closedAccessThiosemicarbazideThiazoleAnticancerTopoisomeraseDocking StudyBiological EvaluationTargetsStrandArticle1302N/AWOS:0011583117000012-s2.0-85181941521Q2