Identification of potent ITK inhibitors through focused compound library design including structural information

…, FU Bosch, G Quintini, C Scheipers, A Weber

文献索引：Herdemann, Matthias; Heit, Isabelle; Bosch, Frank-Uwe; Quintini, Gianluca; Scheipers, Claudia; Weber, Alexander Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 23 p. 6998 - 7003

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被引用次数: 11

摘要

A series of novel compound libraries inhibiting interleukin-2 inducible T cell kinase (ITK) were designed, synthesized and evaluated. In the first design cycle two library scaffolds were identified showing low micromolar inhibition of ITK. Further iterative design cycles including crystal structure information of ITK and structurally related kinases led to the identification of indolylindazole and indolylpyrazolopyridine compounds with low ...