Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase

被引：15

作者：

Zhu, Peiqing ^{[1
]}

Bi, Yi ^{[1
]}

Xu, Jinyi ^{[1
]}

Li, Zan ^{[2
]}

Liu, Jun ^{[3
]}

Zhang, Luyong ^{[3
]}

Ye, Wencai ^{[4
]}

Wu, Xiaoming ^{[2
]}

机构：

[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China

[2] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210038, Peoples R China

[3] China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Peoples R China

[4] China Pharmaceut Univ, Dept Phytochem, Nanjing 210038, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 24期

关键词：

23-Hydroxybetulinic acid; Glycogen phosphorylase inhibitor; Biological evaluation; SAR; BINDING;

D O I：

10.1016/j.bmcl.2009.10.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 23-hydroxybetulinic acid derivatives were prepared and tested in vitro as a new class of inhibitors of glycogen phosphorylase (GP). Within this series of compounds, 12b (IC50 = 3.5 mu M) is the most potent GPa inhibitor. The preliminary SAR results of the 23-hydroxybetulinic acid derivatives are discussed. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6966 / 6969

页数：4

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