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

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Abstract 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… Click to show full abstract

Abstract 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 s-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 s-Catenin was observed, suggesting that the high antitumor potency of 3a may result, in part, from its ability to bind s-Catenin; in addition to other known quinoline mechanisms. This property may be exploited to design future quinoline therapeutic strategies targeting s-Catenin related diseases such as colorectal cancer.

Keywords: quinoline derivative; colorectal cancer; water logsy

Journal Title: Journal of Molecular Structure
Year Published: 2021

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