Synthesis, Characterization and Molecular Docking Studies of Highly Selective New Hydrazone Derivatives of Anthranilic Acid and Their Ring Closure Analogue Quinazolin-4(3H)-ones Against Lung Cancer Cells A549
Yazarlar (4)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Halil Şenol Bezmiâlem Vakıf Üniversitesi, Türkiye
Şeyma Bulut Bezmiâlem Vakıf Üniversitesi, Türkiye
Ebru Hacıosmanoğlu-Aldoğan Bezmiâlem Vakıf Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Journal of Molecular Structure (Q2)
Dergi ISSN 0022-2860 Dergi Bilgileri (2023)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 06-2023
Cilt / Sayı / Sayfa 1282 / 1 / 135176–0 DOI 10.1016/j.molstruc.2023.135176
Makale Linki http://dx.doi.org/10.1016/j.molstruc.2023.135176
UAK Araştırma Alanları
Organik Kimya Spektroskopi Biyokimya
Özet
In this study, new Schiff bases derived from anthranilic acid hydrazide (3a-j) and quinazolin-4(3H)-one (4a-j) were synthesized with high yields (99-90%) and characterized by FTIR, NMR (1H and 13C), and HRMS spectroscopic techniques. The effects of the synthesized compounds on the human lung adenocarcinoma cells (A549, CCL-185, ATCC) and the human bronchial epithelial cells (BEAS-2B, ECACC) were examined. IC50 values of the compounds were found in the range of 12.40 – 424.9 µM against A549 and 15.81 – 752.30 µM against BEAS-2B cell lines. Compounds 3i, 3j, 4b, and 4f are the most active compounds in the series, with low IC50 values against A549, high against BEAS-2B, and high selectivity. For the most active compounds in the series, molecular docking study was performed to understand ligand-protein interactions between the compounds and Epidermal Growth Factor Receptor (EGFR …
Anahtar Kelimeler
Anthranilic acid | Anticancer | Molecular docking | Quinazolin-4(3H)-one, Synthesis