Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization

被引：37
|
作者：
Tasler, Stefan [1 ]
Mueller, Oliver [1 ]
Wieber, Tanja [1 ]
Herz, Thomas [1 ]
Pegoraro, Stefano [1 ]
Saeb, Wael [1 ]
Lang, Martin [1 ]
Krauss, Rolf [1 ]
Totzke, Frank [2 ]
Zirrgiebel, Ute [2 ]
Ehlert, Jan E. [2 ]
Kubbutat, Michael H. G. [2 ]
Schaechtele, Christoph [2 ]
机构：
[1] 4SC AG, D-82152 Planegg Martinsried, Germany
[2] ProQinase GmbH, D-79106 Freiburg, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 18期
关键词：
Cancer; Protein kinase; vHTS; Multi-target approach; RECEPTOR TYROSINE KINASE; BREAST-CANCER CELLS; POTENT; IDENTIFICATION; DISCOVERY; THERAPY; COMPLEX; TARGETS; DESIGN; DOMAIN;
D O I：
10.1016/j.bmc.2009.07.047
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：
Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6728 / 6737
页数：10
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