KKB Hot Article: Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.

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KKB Hot Article: Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.

Written by KKB

Tuesday, 20 April 2010 19:46

Citation: Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.

Authors: Tasler S, Müller O, Wieber T, Herz T, Pegoraro S, Saeb W, Lang M, Krauss R, Totzke F, Zirrgiebel U, Ehlert JE, Kubbutat MH, Schächtele C.

PubMed PMID: 19692247

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.

Targets: AURKA, AURKB, EGFR, ERBB2, FLT4, KDR, PDGFRB, TEK
Number of SAR data points: 204
Number of Targets: 8

Last Updated on Saturday, 20 August 2011 00:05

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