@article{APS3895,
author = {Hai-hong Li and He Huang and Xiu-hua Zhang and Xiao-min Luo and Li-ping Lin and Hua-liang Jiang and Jian Ding and Kaixian Chen and Hong Liu},
title = {Discovering novel 3-nitroquinolines as a new class of anticancer agents},
journal = {Acta Pharmacologica Sinica},
volume = {29},
number = {12},
year = {2016},
keywords = {},
abstract = {Aim: To design and synthesize a novel class of antitumor agents, featuring the 3-nitroquinoline framework.
Methods: Based on the enzyme-binding features of Ekb1, introducing a nitro group at the 3-position of the quinoline core, a series of novel 3-nitroquinolines was designed and synthesized. The inhibition of epidermal growth factor receptor (EGFR) activity by these compounds was evaluated and analyzed by the sulforhodamine B assay for their inhibitory activities toward human epidermoid carcinoma (A431) cells and breast cancer (MDA-MB-468) cells, which are known to overexpress the EGFR kinase.
Results: A series of novel 3-nitroquinoline derivatives were synthesized and evaluated for their antiproliferative effect against the EGFR-overexpressing tumor cell lines. Several compounds for concentration-response studies showed prominent inhibitory activities with IC50 values in the micromolar or nanomolar range. The structure-activity relationship was discussed in terms of the inhibitory activity against the proliferation of 2 human carcinoma cell lines.
Conclusion: This study was the first to identify new structural types of antiproliferative agents against the EGFR-overexpressing tumor cell lines by the incorporation of the nitro group at the 3-position of the quinoline core structure, providing promising new templates for the further development of anticancer agents.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/3895}
}