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Design, Synthesis, and In Silico and In Vitro Cytotoxic Activities of Novel Isoniazid-Hydrazone Analogues Linked to Fluorinated Sulfonate Esters

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dc.creator Tür, Gulal
dc.creator AKKOÇ, Senem
dc.creator Başaran, Eyüp
dc.creator Taskin-Tok, Tugba
dc.date 2024-01-01T00:00:00Z
dc.date.accessioned 2025-02-25T10:34:48Z
dc.date.available 2025-02-25T10:34:48Z
dc.identifier 9a214467-ed79-4574-9e69-07858befb67c
dc.identifier 10.1021/acsomega.4c00652
dc.identifier https://avesis.sdu.edu.tr/publication/details/9a214467-ed79-4574-9e69-07858befb67c/oai
dc.identifier.uri http://acikerisim.sdu.edu.tr/xmlui/handle/123456789/100683
dc.description Cancer is a life-threatening disease, and significant efforts are still being made to treat it. In this study, we synthesized and characterized novel hybrid molecules (10-18) containing hydrazone and sulfonate moieties and tested their cell growth inhibitory effect on human colon cancer cells (DLD-1), human prostate cancer cells (PC3), and human embryonic kidney cells (HEK-293T) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method for 72 h. In cell culture studies, all tested hybrid molecules except for 12 and 13 showed significant cytotoxic activities at a micromolar level with IC50 values in the range of 10.28-214.0 μM for the PC3 cell line and 13.49-144.30 μM for the DLD-1 cell line. Compounds 4 (10.28 μM) and 5 (11.22 μM) demonstrated the highest cytotoxicity against the PC3 cell line. Against the DLD-1 cell line, compounds 1 (22.53 μM), 4 (13.49 μM), 5 (19.33 μM), 6 (17.82 μM), 8 (24.71 μM), 9 (17.56 μM), and 10 (17.90 μM) in the series showed anticancer activity at lower micromolar levels compared to cisplatin (26.70 μM). Moreover, the study was handled computationally, and molecular docking studies were performed for compounds 1, 4, and 5 for PC3-FAK and PC3-Scr and compounds 4, 6, and 9 for the DLD-1-TNKS target. In this study, compound 4 was found to be the most effective and promising molecule for both targets.
dc.language eng
dc.rights info:eu-repo/semantics/closedAccess
dc.title Design, Synthesis, and In Silico and In Vitro Cytotoxic Activities of Novel Isoniazid-Hydrazone Analogues Linked to Fluorinated Sulfonate Esters
dc.type info:eu-repo/semantics/article


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