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

S Tasler, O Müller, T Wieber, T Herz, S Pegoraro…

Index: Tasler, Stefan; Mueller, Oliver; Wieber, Tanja; Herz, Thomas; Pegoraro, Stefano; Saeb, Wael; Lang, Martin; Krauss, Rolf; Totzke, Frank; Zirrgiebel, Ute; Ehlert, Jan E.; Kubbutat, Michael H.G.; Schaechtele, Christoph Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 18 p. 6728 - 6737

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Citation Number: 27

Abstract

Download PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... 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. ... Arylbenzothiazole derivatives originating from a ...