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Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization. 2009
Stefan Tasler, and
Oliver Müller, and
Tanja Wieber, and
Thomas Herz, and
Stefano Pegoraro, and
Wael Saeb, and
Martin Lang, and
Rolf Krauss, and
Frank Totzke, and
Ute Zirrgiebel, and
Jan E Ehlert, and
Michael H G Kubbutat, and
Christoph Schächtele
4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany.
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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