Structure Modification of FXR Antagonistic Chalcones and Their Inhibitory Effects on NSCLC Cell Proliferation and Metastasis
CHEMMEDCHEM(2022)
摘要
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.
更多查看译文
关键词
chalcone,FXR antagonist,Antiproliferation,NSCLC
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要