Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species:: Novel inhibitors of protein kinases
Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species:: Novel inhibitors of protein kinases
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DOI：
10.1021/np9905259
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发表时间：
2000-06-01
影响因子：
5.1
通讯作者：
Schaumann, K
中科院分区：
文献类型：
--
作者：
Brauers, G;Edrada, RA;Schaumann, K
从地中海海绵Aplysina aerophoba中分离出的一种未描述的拟微球菌属真菌产生两种新的β烯酮衍生物（1，2）和三种新的1，3，6，8-四羟基蒽醌同系物（5-7）。基于NMR光谱和质谱数据以及通过CD光谱确定化合物的结构。这是第一份报告，其中的β烯酮同系物的H-1和C-13 NMR数据是完全和明确的基础上分配的二维NMR光谱。此外，我们描述了1-（2 '-蒽醌基）乙醇，如5和6的绝对构型的量子化学计算的圆二色性（CD）和实验测量的光谱比较。此外，显示化合物1、5、6和7是PKC-ERK、CDK 4和EGF受体酪氨酸激酶的抑制剂。
An undescribed fungus of the genus Microsphaeropsis, isolated from the Mediterranean sponge Aplysina aerophoba, produces two new betaenone derivatives (1, 2) and three new 1,3,6,8-tetrahydroxyanthraquinone congeners (5-7). The structures of the compounds were established on the basis of NMR spectroscopic and mass spectrometric data and by CD spectroscopy. This is the first report wherein the H-1 and C-13 NMR data of the betaenone congeners are fully and unambiguously assigned on the basis of two-dimensional NMR spectroscopy. Furthermore, we describe the first elucidation of the absolute configuration of 1-(2'-anthraquinonyl)ethanols such as 5 and 6, by quantum chemical calculation of their circular dichroism (CD) and comparison with experimentally measured spectra. Moreover, it was shown that compounds 1, 5, 6, and 7 are inhibitors of PKC-epsilon, CDK4, and EGF receptor tyrosine kinases.