In colorectal cancer; NMR-monitored β-Catenin inhibition by a Quinoline derivative using Water-LOGSY technique

2-Amino-4-(2-chloroquinolin-3-yl)-7-hydroxy-4H-chromene-3-carbonitrile (3a) is a quinoline derivative that has been shown to possess antitumor activity. Beside activity, the compound has reasonable solubility in aqueous buffers. Herein, we tested its activity as potential ligand for ß-Catenin protei...

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Veröffentlicht in:Journal of molecular structure 2021-12, Vol.1246, p.131151, Article 131151
Hauptverfasser: Mansour, Basem, Henen, Morkos A., Bayoumi, Waleed A., El-Sayed, Magda A., Massoud, Mohammed A.M.
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Sprache:eng
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Zusammenfassung:2-Amino-4-(2-chloroquinolin-3-yl)-7-hydroxy-4H-chromene-3-carbonitrile (3a) is a quinoline derivative that has been shown to possess antitumor activity. Beside activity, the compound has reasonable solubility in aqueous buffers. Herein, we tested its activity as potential ligand for ß-Catenin protein as molecular target. We used Water-LOGSY NMR as our method of choice to test the binding. A selective binding of 3a to ß-Catenin was observed, suggesting that the high antitumor potency of 3a may result, in part, from its ability to bind ß-Catenin; in addition to other known quinoline mechanisms. This property may be exploited to design future quinoline therapeutic strategies targeting ß-Catenin related diseases such as colorectal cancer.
ISSN:0022-2860
1872-8014
DOI:10.1016/j.molstruc.2021.131151