New Anthranilic Acid Hydrazones as Fenamate Isosteres: Synthesis, Characterization, Molecular Docking, Dynamics & in silico ADME, in vitro Anti‐inflammatory and Anti‐cancer Activity Studies
 
Yazarlar (4)
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Dr. Öğr. Üyesi Zeynep Çağman Bezmiâlem Vakıf Üniversitesi, Türkiye
Tuğba Gençoğlu Katmerlikaya
Bezmiâlem Vakıf Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Chemistry and Biodiversity (Q3)
Dergi ISSN 1612-1872 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 08-2023
Cilt / Sayı / Sayfa 20 / 8 / 1–16 DOI 10.1002/cbdv.202300773
Makale Linki http://dx.doi.org/10.1002/cbdv.202300773
UAK Araştırma Alanları
Organik Kimya Spektroskopi Biyokimya
Özet
In this study, twenty new anthranilic acid hydrazones 6–9 (a–e) were synthesized and their structures were characterized by Fourier‐transform Infrared (FT‐IR), Nuclear Magnetic Resonance (1H‐NMR – 13C‐NMR), and High‐resolution Mass Spectroscopy (HR‐MS). The inhibitory effects of the compounds against COX‐II were evaluated. IC50 values of the compounds were found in the range of >200–0.32 μM and compounds 6e, 8d, 8e, 9b, 9c, and 9e were determined to be the most effective inhibitors. Cytotoxic effects of the most potent compounds were investigated against human hepatoblastoma (Hep‐G2) and human healthy embryonic kidney (Hek‐293) cell lines. Doxorubicin (IC50: 8.68±0.16 μM for Hep‐G2, 55.29±0.56 μM for Hek‐293) was used as standard. 8e is the most active compound, with low IC50 against Hep‐G2 (4.80±0.04 μM), high against Hek‐293 (159.30±3.12), and high selectivity (33.15 …
Anahtar Kelimeler
ADME | anti-cancer | anti-inflammatory | molecular docking | molecular dynamics