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Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives

   
@article{APS3957,
	author = {Jian Li and Jin-zhi Tan and Li-li Chen and Jian Zhang and Xu Shen and Chang-lin Mei and Li-li Fu and Li-ping Lin and Jian Ding and Bing Xiong and Xi-shan Xiong and Hong Liu and Xiao-min Luo and Hua-liang Jiang},
	title = {Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives},
	journal = {Acta Pharmacologica Sinica},
	volume = {27},
	number = {9},
	year = {2016},
	keywords = {},
	abstract = {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 (1–2, 3a–g, 4a–w, and 5a–l) 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 activity.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/3957}
}