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 frst 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. © 2008 CPS and SIMM.
CITATION STYLE
Li, H. H., Huang, H., Zhang, X. H., Luo, X. M., Lin, L. P., Jiang, H. L., … Liu, H. (2008). Discovering novel 3-nitroquinolines as a new class of anticancer agents. Acta Pharmacologica Sinica, 29(12), 1529–1538. https://doi.org/10.1111/j.1745-7254.2008.00907.x
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