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  • Targeting DNA Binding for NF-kappa B as an Anticancer Approach in Hepatocellular Carcinoma

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    Author(s)
    Chung, Po Yee
    Lam, Pik Ling
    Zhou, Yuanyuan
    Gasparello, Jessica
    Finotti, Alessia
    Chilin, Adriana
    Marzaro, Giovanni
    Gambari, Roberto
    Bian, Zhaoxiang
    Kwok, Wai Ming
    Wong, Wai Yeung
    Wang, Xi
    Lam, Alfred King-yin
    Chan, Albert Sun-chi
    Li, Xingshu
    Ma, Jessica Yuen Wuen
    Chui, Chung Hin
    Lam, Kim Hung
    Tang, Johnny Cheuk On
    Griffith University Author(s)
    Lam, Alfred K.
    Year published
    2018
    Metadata
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    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 ...
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    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-κB to its target DNA. Accordingly, compound 5 represented a lead structure for the development of quinoline-based NF-κB inhibitors and this work added novel information on the understanding of the mechanism of action for bioactive sulfonyl-containing quinoline compounds against hepatocellular carcinoma.
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    Journal Title
    Cells
    Volume
    7
    Issue
    10
    DOI
    https://doi.org/10.3390/cells7100177
    Copyright Statement
    © 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 (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
    Subject
    Gastroenterology and hepatology
    Oncology and carcinogenesis
    Cancer genetics
    Science & Technology
    Life Sciences & Biomedicine
    Cell Biology
    NF-kappa B
    anticancer
    Publication URI
    http://hdl.handle.net/10072/387910
    Collection
    • Journal articles

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