Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2

被引：8

作者：

Ashton, Kate S. ^{[1
]}

St Jean, David J., Jr. ^{[1
]}

Poon, Steve F. ^{[1
]}

Lee, Matthew R. ^{[1
]}

Allen, John G. ^{[1
]}

Zhang, Shiwen ^{[2
]}

Lofgren, Julie A. ^{[2
]}

Zhang, Xiaoling ^{[2
]}

Fotsch, Christopher ^{[1
]}

Hungate, Randall ^{[1
]}

机构：

[1] Amgen Inc, Chem Res & Discovery, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Oncol Res, Thousand Oaks, CA 91320 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 18期

关键词：

PKB; AKT; CDK; Cancer; PROTEIN-KINASE-B; PI3K/AKT PATHWAY; RECENT PROGRESS; CANCER; IDENTIFICATION; DISCOVERY; BINDING; AKT/PKB; TUMORIGENESIS;

D O I：

10.1016/j.bmcl.2011.07.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Through the analysis of X-ray crystallographic information and previous SAR studies, a novel series of protein kinase B (PKB/AKT) inhibitors was developed. The compounds showed nanomolar inhibition of AKT1 and were selective against cyclin-dependent kinase 2 (CDK2). (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5191 / 5196

页数：6

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