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

DOI: 10.1016/j.bmc.2009.07.047

Source and publish data:

Bioorganic and Medicinal Chemistry p. 6728 - 6737 (2009)

Update date:2022-08-05

Topics:

Authors:

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

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Article abstract of DOI:10.1016/j.bmc.2009.07.047

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.

Full text of DOI:10.1016/j.bmc.2009.07.047

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