Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: Design, synthesis and biological activity
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: Design, synthesis and biological activity
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DOI：
10.1016/j.bmcl.2007.04.071
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发表时间：
2007-07-15
影响因子：
2.7
通讯作者：
Arnaiz, Damian O.
中科院分区：
文献类型：
--
作者：
Islam, Imadul;Bryant, Judi;Arnaiz, Damian O.
HTS筛选鉴定了对PDK 1具有微摩尔抑制活性的I。优化1得到4 i（BX-517），其对PDK 1具有单位纳摩尔活性，对PKA具有优异的选择性。(C)2007爱思唯尔有限公司保留所有权利。
HTS screening identified I with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA. (C) 2007 Elsevier Ltd. All rights reserved.