作为激酶抑制剂的取代2-芳基苯并噻唑：从活性化合物到先导化合物的优化
Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.
作者信息
Tasler Stefan, Müller Oliver, Wieber Tanja, Herz Thomas, Pegoraro Stefano, Saeb Wael, Lang Martin, Krauss Rolf, Totzke Frank, Zirrgiebel Ute, Ehlert Jan E, Kubbutat Michael H G, Schächtele Christoph
机构信息
4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany.
出版信息
Bioorg Med Chem. 2009 Sep 15;17(18):6728-37. doi: 10.1016/j.bmc.2009.07.047. Epub 2009 Jul 25.
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.
摘要
基于用于激酶抑制的（氨基芳基）苯并噻唑喹唑啉命中结构，一个系统的优化程序产生了一种先导结构，该结构在细胞磷酸化测定中具有低纳摩尔范围内的抑制活性。
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