586330-18-9Relevant academic research and scientific papers
Optimisation of ITK inhibitors through successive iterative design cycles
Herdemann, Matthias,Weber, Alexander,Jonveaux, Jér?me,Schwoebel, Frank,Stoeck, Michael,Heit, Isabelle
scheme or table, p. 1852 - 1856 (2011/05/05)
Based on a hit cluster of compounds inhibiting interleukin-2 inducible T-cell kinase (ITK) in the submicromolar range a series of ITK inhibitor libraries were synthesized. Through iterative design cycles including kinase crystal structure information, indolylindazole libraries were identified which showed low nanomolar activity in enzymatic and cellular assays. The potential of these novel lead series was confirmed through in vivo tests in an anti-CD3-IL2 mouse model. The intravenous administration of highly potent ITK inhibitor 11o resulted in dose-dependent, efficient suppression of IL-2.
p38 MAP kinase inhibitors and methods for using the same
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Page/Page column 24, (2008/06/13)
Compounds of formula Ia or Ib: wherein X and Y are nitrogen or CRe, and R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the subject compounds and methods o
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3
Swahn, Britt-Marie,Huerta, Fernando,Kallin, Elisabet,Malmstroem, Jonas,Weigelt, Tatjana,Viklund, Jenny,Womack, Patrick,Xue, Yafeng,Oehberg, Liselotte
, p. 5095 - 5099 (2007/10/03)
The structure-based design and synthesis of a new series of c-Jun N-terminal kinase-3 inhibitors with selectivity against JNK1 and p38α is reported. The novel series of substituted 6-anilinoindazoles were designed based on a combination of hits from high
