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Structure Modification of FXR Antagonistic Chalcones and Their Inhibitory Effects on NSCLC Cell Proliferation and
Shuaishuai Niu1,2, Guoning Zhang2, Na Wang3,4
1Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery Systems and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, China.
None:
Although the farnesoid X receptor (FXR) has been regarded as a promising drug target for metabolic diseases as well as anti-inflammatory, antitumor and antiviral actions, the antagonism by FXR ligands are still underrepresented in current FXR targeted therapies. In this study, we discovered selective FXR antagonists through structure optimization from the polyoxygenated chalcone scaffold. The selective antagonist 6 p [2-methoxy-2'-hydroxy-4'-(4''-methoxy-4''-oxo-E-crotonyl) chalcone] is not only inhibitory toward non-small-cell lung cancer (NSCLC) cell proliferation in an FXR-dependent manner, but is also active in metastasis models. Taken together, this chalcone-based FXR antagonist has the potential for the targeted therapy of NSCLC in which FXR is highly expressed.
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