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Akademisyenler > Musa ERDOĞAN > Yayın Detayı

Sulfonyl Hydrazone Derivatives Targeting Glutathione Reductase: A Potential Strategy for Redox Modulation in Cancer      
Yazarlar (6)
Doç. Dr. Erbay KALAY Doç. Dr. Erbay KALAY
Kafkas Üniversitesi, Türkiye
Halide Sedef Karaman
Atatürk Üniversitesi, Türkiye
Osman Nuri Aslan
Atatürk Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Doç. Dr. Feyzi Sinan TOKALI
Kafkas Üniversitesi, Türkiye
Muhammet Karaman
Dokuz Eylül Üniversitesi, Türkiye
Doç. Dr. Musa ERDOĞAN Doç. Dr. Musa ERDOĞAN
Kafkas Üniversitesi, Türkiye
Devamını Göster
Özet
Glutathione reductase (GR) plays a pivotal role in cellular metabolism by maintaining redox balance and sulfhydryl homeostasis through the regeneration of reduced glutathione (GSH). In tumor cells, GR is overexpressed, supporting enhanced antioxidant defenses and neutralizing the detrimental effects of reactive oxygen species. In this study, a series of sulfonyl hydrazone analogs bearing phenolic Mannich base moieties were synthesized and characterized as potential GR inhibitors. The compounds exhibited inhibitory activity with IC50 values ranging from 198.1 to 3013 nM. In silico analyses revealed that 6a binds to the NADP+ binding site of the hGR enzyme and interacts with key residues involved in electron transfer, leading to reduced enzyme activity. Compound 6a, the most potent hGR enzyme inhibitor identified in this study, exhibited cytotoxic effects against MCF-7, A549, and HeLa cancer cell lines with EC50 values of ~1.52, ~17.5, and ~8.82 mM, respectively. Notably, compound 6a demonstrated only weak cytotoxicity at the millimolar level, particularly against the MCF-7 cell line. Given its strong inhibitory activity toward the hGR enzyme, enhancing the membrane permeability of compound 6a may improve its cellular uptake and potency, thereby supporting its potential as a promising anticancer drug candidate.
Anahtar Kelimeler
cell viability | enzyme inhibition | glutathione reductase | molecular docking | sulfonyl hydrazone
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Chemical Biology and Drug Design
Dergi ISSN 1747-0277 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q2
Makale Dili Türkçe
Basım Tarihi 11-2025
Cilt No 106
Sayı 5
Doi Numarası 10.1111/cbdd.70198
Makale Linki https://doi.org/10.1111/cbdd.70198
BM Sürdürülebilir Kalkınma Amaçları
Atıf Sayıları
Sulfonyl Hydrazone Derivatives Targeting Glutathione Reductase: A Potential Strategy for Redox Modulation in Cancer

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