Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors

被引：11

作者：

Meng, Zhaoyang ^{[1
]}

Ciavarri, Jeffrey P. ^{[1
]}

McRiner, Andrew ^{[1
]}

Zhao, Yinyan ^{[1
]}

Zhao, Lianyun ^{[1
]}

Reddy, Panduranga Adulla ^{[1
]}

Zhang, Xingmin ^{[1
]}

Fischmann, Thierry O. ^{[2
]}

Whitehurst, Charles ^{[1
]}

Siddiqui, M. Arshad ^{[1
]}

机构：

[1] Merck Res Labs, Cambridge, MA 02141 USA

[2] Merck Res Labs, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 10期

关键词：

Potency switch; CHK1; MK2; Kinase; Inhibitor; DNA-DAMAGE RESPONSE; CHECKPOINT KINASE; CELL-CYCLE; ATR;

D O I：

10.1016/j.bmcl.2013.03.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Chemistry has been developed to access both imidazo[1,2-a]pyrazines and imidazo[1,2-c]pyrimidines. Small structural modifications in both series led to a switch of potency between two kinases involved in mediating cell cycle checkpoint control, CHK1 and MK2. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：2863 / 2867

页数：5

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