Aim: To design and synthesize a novel class of protein tyrosine kinase inhibitors,
featuring the N-(2-oxo-1,2-dihydroquinolin-3-yl-methyl)-thiourea framework.
Methods: First, compounds 1 and 2 were identified using the virtual screening
approach in conjunction with binding assay based on surface plasmon resonance.
Subsequently, 3 regions of compounds 1 and 2 were selected for chemical modification.
All compounds were characterized potent inhibitory activities toward the
human lung adenocarcinoma cell line SPAC1. Results: Forty new compounds (1¨C
2, 3a¨Cg, 4a¨Cw, and 5a¨Cl) were designed, synthesized and bioassayed. Six compounds
(1, 3e, 4l, 4w, 5a, and 5b) were found to show promising inhibitory activity
against the SPAC1 tumor cell line. The inhibitory activity of compound 5a
increases approximately 10 times more than that of the original compound 1.
Conclusion: This study provides a promising new template with potential antitumor