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Title: Targeting DNA binding for NF-kappa B as an anticancer approach in hepatocellular carcinoma
Authors: Chung, PY 
Lam, PL 
Zhou, YY 
Gasparello, J
Finotti, A
Chilin, A
Marzaro, G
Gambari, R
Bian, ZX
Kwok, WM 
Wong, WY 
Wang, X 
Lam, AKY
Chan, ASC
Li, XS
Ma, JYW 
Chui, CH 
Lam, KH 
Tang, JCO 
Keywords: NF-kappa B
Hepatocellular carcinoma
Issue Date: 2018
Publisher: Molecular Diversity Preservation International (MDPI)
Source: Cells, Oct. 2018, v. 7, no. 10, 177, p. 1-14 How to cite?
Journal: Cells 
Abstract: Quinoline core has been shown to possess a promising role in the development of anticancer agents. However, the correlation between its broad spectrum of bioactivity and the underlying mechanism of actions is poorly understood. The present study, with the use of bioinformatics approaches, reported a series of designed molecules which integrated quinoline core and sulfonyl moiety, with the objective of evaluating the substituent and linker effects on anticancer activities and associated mechanistic targets. We identified potent compounds (1h, 2h, 5 and 8) exhibiting significant anticancer effects towards liver cancer cells (Hep3B) with the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) relative values of cytotoxicity below 0.40, a value in the range of doxorubicin positive control with the value of 0.12. Bulky substituents and the presence of bromine atom, as well as the presence of sulfonamide linkage, are likely the favorable structural components for molecules exerting a strong anticancer effect. To the best of our knowledge, our findings obtained from chemical synthesis, in vitro cytotoxicity, bioinformatics-based molecular docking analysis (similarity ensemble approach, SEA),and electrophoretic mobility shift assay provided the first evidence in correlation to the anticancer activities of the selected compound 5 with the modulation on the binding of transcription factor NF-kappa B to its target DNA. Accordingly, compound 5 represented a lead structure for the development of quinoline-based NF-kappa B inhibitors and this work added novel information on the understanding of the mechanism of action for bioactive sulfonyl-containing quinoline compounds against hepatocellular carcinoma.
DOI: 10.3390/cells7100177
Rights: © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (
The following publication Chung, P.Y., Lam, P.L., Zhou, Y.Y., Gasparello, J., Finotti, A., Chilin, A., ... & Tang, J.C.O. (2018). Targeting DNA binding for NF-kappa B as an anticancer approach in hepatocellular carcinoma. Cells, 7 (10), 177, p. 1-14 is available at
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