2022
DOI: 10.1002/cmdc.202100778
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Structure Modification of FXR Antagonistic Chalcones and Their Inhibitory Effects on NSCLC Cell Proliferation and Metastasis

Abstract: Although the farnesoid X receptor (FXR) has been regarded as a promising drug target for metabolic diseases as well as antiinflammatory, 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 towa… Show more

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