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来自……的酰基间苯三酚作为激酶抑制剂

Acylphloroglucinols as kinase inhibitors from .

作者信息

Jiang Cheng-Shi, Wang Yin-Yin, Song Jin-Tong, Yu Jin-Hai

机构信息

a School of Biological Science and Technology , University of Jinan , Jinan 250022 , China.

出版信息

J Asian Nat Prod Res. 2019 Jul;21(7):619-626. doi: 10.1080/10286020.2018.1463996. Epub 2018 May 28.

Abstract

Three new acylphloroglucinols (-) and four known biosynthetically related analogs (-) were isolated from the ethanol extract of a brown alga . Structures for - were characterized detailed spectroscopic analyses especially 2D NMR data. Screening of these compounds in Alzheimer's diseases-related bioassays revealed moderate inhibitory activities against two therapeutically important kinases, CDK5 and GSK3β. A preliminary structure-activity relationship was also discussed.

摘要

从一种褐藻的乙醇提取物中分离出三种新的酰基间苯三酚(-)和四种已知的生物合成相关类似物(-)。通过详细的光谱分析,尤其是二维核磁共振数据对-的结构进行了表征。在与阿尔茨海默病相关的生物测定中对这些化合物进行筛选,结果显示它们对两种具有重要治疗意义的激酶CDK5和GSK3β具有中等抑制活性。还讨论了初步的构效关系。

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