Synthesis, Characterization, In Vitro and In Silico Investigations of Novel 1,2,3-Triazole Substituted Salicylic Acid Phenolic-Hydrazones Hybrids Targeting TGF-β2 Expression in Colorectal Carcinoma
 
Yazarlar (6)
Ebru Nur Ay İstinye Üniversitesi, Türkiye
Arş. Gör. Furkan Çakır Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Sarehan Akyüz Yıldız Teknik Üniversitesi, Türkiye
Doç. Dr. Namık Kılınç Iğdır Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı European Journal of Medicinal Chemistry (Q1)
Dergi ISSN 0223-5234 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 10-2025
Cilt / Sayı / Sayfa 296 / 1 / 117915–0 DOI 10.1016/j.ejmech.2025.117915
Makale Linki https://doi.org/10.1016/j.ejmech.2025.117915
UAK Araştırma Alanları
Organik Kimya
Özet
In this study, sixteen novel 1,2,3-triazole-substituted salicylic acid phenolic-hydrazone hybrids were synthesized and characterized using NMR, IR, HRMS, and HPLC techniques. The compounds were evaluated for their anticancer potential against HCT-116, Caco-2 and HT-29 colorectal carcinoma cells and normal BEAS-2B epithelial cells. Among them, compound 10k exhibited potent antiproliferative effects on HCT-116, Caco-2 and HT-29 with IC50 values of 6.84, 10.21, and 9.47 μM, respectively, which were significantly lower than the reference drug sorafenib (IC50 = 18.25, 13.80 and 7.89 μM) for HTC-116 and Caco-2. Biological assays demonstrated that 10k effectively downregulated TGF-β2 receptor and cytokine expression in a dose-dependent manner, indicating its role in modulating the TGF-β signaling pathway. Apoptosis analysis suggested that cytotoxicity was mediated via non-apoptotic mechanisms …
Anahtar Kelimeler
1,2,3-Triazoles | Colorectal cancer | Hydrazone | Molecular docking | TGF-β2