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In silico identification and in vitro validation of nogalamycin N-oxide (NSC116555) as a potent anticancer compound against non–small-cell lung cancer cells
Author(s)
Obounchoey, Phongphat
Tabtimmai, Lueacha
Suphakun, Praphasri
Thongkhao, Kannika
Eurtivong, Chatchakorn
Gleeson, Matthew Paul
Choowongkomon, Kiattawee
Date Issued
March 1, 2019
Type
Article
Abstract
The epidermal growth factor receptor (EGFR) was found to be overexpressed in several cancers, especially in lung cancers. Finding new effective drug against EGFR is the key to cancer treatment. In this study, the GOLD docking algorithm was used to virtually screen for novel human EGFR inhibitors from the NCI database. Thirty-four hit compounds were tested for EGFR-tyrosine kinase (TK) inhibition. Two potent compounds, 1-amino-4-(4-[4-amino-2-sulfophenyl]anilino)-9,10-dioxoanthracene-2-sulfonic acid (NSC125910), and nogalamycin N-oxide (NSC116555) were identified with IC 50 values against EGFR-TK comparable to gefitinib; 16.14 and 37.71 nM, respectively. However, only NSC116555 demonstrated cytotoxic effects against non–small-cell lung cancer, A549, shown in the cell cytotoxicity assay with an IC 50 of 0.19 + 0.01 µM, which was more potent than gefitinib. Furthermore, NSC116555 showed cytotoxicity against A549 via apoptosis in a dose-dependent manner.
Citation
Journal of Cellular Biochemistry, 120(3), 3353-3361, 2019