Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization |
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| Authors: | Stefan Tasler, Oliver Mü ller, Tanja Wieber, Thomas Herz, Stefano Pegoraro, Wael Saeb, Martin Lang, Rolf Krauss, Frank Totzke, Ute Zirrgiebel, Jan E. Ehlert, Michael H.G. Kubbutat,Christoph Sch chtele |
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| Affiliation: | a4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany;bProQinase GmbH, Breisacher Str. 117, 79106 Freiburg, Germany |
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| Abstract: | 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. |
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| Keywords: | Cancer Protein kinase vHTS Multi-target approach |
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