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
Doç. Dr. Halil Şenol Bezmiâlem Vakıf Üniversitesi, Türkiye
Dr. Öğr. Üyesi 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 Wos Dergi Scopus Dergi
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