Synthesis and biological evaluation of 2-anilino-4-substituted-7H-pyrrolopyrimidines as PDK1 inhibitors

被引：14

作者：

O'Brien, Nathan J. ^{[1
]}

Brzozowski, Martin ^{[1
]}

Buskes, Melissa J. ^{[1
]}

Deady, Leslie W. ^{[1
]}

Abbott, Belinda M. ^{[1
]}

机构：

[1] La Trobe Univ, Dept Chem, La Trobe Inst Mol Sci, Bundoora, Vic 3086, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 15期

关键词：

3-Phosphoinositide-dependent kinase 1 (PDK1); 2-Anilino-4-substituted-pyrrolopyrimidines; Inhibitor; Suzuki cross-coupling; Buchwald-Hartwig cross-coupling; SMALL-MOLECULE INHIBITORS; KINASE; PKB/AKT; PATHWAY;

D O I：

10.1016/j.bmc.2014.06.018

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

PDK1, a biological target that has attracted a large amount of attention recently, is responsible for the positive regulation of the PI3K/Akt pathway that is often activated in a large number of human cancers. A series of second-generation 2-anilino-4-substituted-7H-pyrrolopyrimidines were synthesised by installation of various functions at the 4-position of the 7H-pyrrolopyrimidine scaffold. All compounds were screened against the isolated PDK1 enzyme and dose response analysis was obtained on the best compounds of the series. Crown Copyright (C) 2014 Published by Elsevier Ltd. All rights reserved.

引用

页码：3879 / 3886

页数：8

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