Potent HGF/c-Met Axis Inhibitors from Eucalyptus globulus: the Coupling of Phloroglucinol and Sesquiterpenoid Is Essential for the Activity
Potent HGF/c-Met Axis Inhibitors from Eucalyptus globulus: the Coupling of Phloroglucinol and Sesquiterpenoid Is Essential for the Activity
复制标题
来自蓝桉的有效 HGF/c-Met 轴抑制剂：间苯三酚和倍半萜类化合物的偶联对于活性至关重要
DOI：
10.1021/jm3007454
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发表时间：
2012-09-27
影响因子：
7.3
通讯作者：
Yue, Jian-Min
中科院分区：
文献类型：
--
作者：
Yang, Sheng-Ping;Zhang, Xiao-Wei;Yue, Jian-Min
Eucalyptus globulus的果实中发现了Eucalyptus tin A（1）和两个对HGF/c-Met轴具有有效抑制作用的已知化合物2和3。1具有前所未有的间苯三酚偶联倍半萜碳骨架，通过光谱和电子捕获密度计算确定了其结构。一个简短的构效关系的讨论表明，间苯三酚和倍半萜类化合物的耦合是必不可少的活性。
Eucalyptin A (1), together with two known compounds 2 and 3 exhibiting potent inhibition on HGF/c-Met axis, was discovered from the fruits of Eucalyptus globulus. 1 possessed an unprecedented carbon framework of phloroglucinol-coupled sesquiterpenoid, and its structure was elucidated by spectroscopic method and ECD calculation. A brief structure-activity relationship discussion indicated that the coupling of a phloroglucinol and a sesquiterpenoid is essential for the activity.