alexa Optimisation of ITK inhibitors through successive iterative design cycles.


Journal of Clinical & Cellular Immunology

Author(s): Herdemann M, Weber A, Jonveaux J, Schwoebel F, Stoeck M,

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Abstract 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. Copyright © 2011 Elsevier Ltd. All rights reserved. This article was published in Bioorg Med Chem Lett and referenced in Journal of Clinical & Cellular Immunology

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