Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives

被引：16

作者：

Cui, YM

Huang, QQ

Xu, J

Chen, LL

Li, JY

Ye, QZ

Li, J

Nan, FJ

机构：

[1] Chinese Acad Sci, Shanghai Inst Biol Sci, Grad Sch, Inst Mat Med,Chinese Natl Ctr Drug Screening, Shanghai 201203, Peoples R China

[2] Univ Kansas, High Throughput Screening Lab, Lawrence, KS 66047 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 18期

基金：

中国国家自然科学基金;

关键词：

type I MetAPs inhibitors; bioisosteric replacement;

D O I：

10.1016/j.bmcl.2005.06.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Systematic SAR studies on the thiazole ring 5-substituent of TCAT derivatives revealed that the introduction of a beta-alkoxy or an amino group enhanced the inhibitory activity significantly. The present compounds are representative of specific Co(II)-MetAP1 inhibitors. Before the physiologically relevant metal ions for MetAPs are established, these small molecular compounds could be used as tools for detailed biological studies. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4130 / 4135

页数：6

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