Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK) |
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Authors: | Avdhoot D. Velankar Gianluca Quintini Arati Prabhu Alexander Weber Gundula Hunaeus Britta Voland Monika Wuest Christian Orjeda Dipak Harel Shaji Varghese Vikas Gore Meenal Patil Deepak Gayke Matthias Herdemann Isabelle Heit Andrea Zaliani |
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Affiliation: | 1. Global Discovery, Nycomed Pharma Pvt. Ltd, Plot number 29-30-31, Suren Road, Andheri (East), Mumbai 400 093, Maharashtra, India;2. Global Discovery, Nycomed GmbH, Byk-Gulden-Str 2, 78467 Konstanz, Germany |
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Abstract: | Interleukin-2 inducible T-cell kinase (ITK) is one of five kinases that belong to the Tec kinase family that plays an important role in T-cell and mast cell signaling. Various reports point to a role of ITK in the treatment of allergic asthma. For example, it was shown that mice lacking ITK have reduced airway hyperresponsiveness, inflammation and tracheal responses in an allergic asthma model. In this article, we disclose novel ITK inhibitors based on (4 or 5-aryl)pyrazolyl-indole scaffold that were also found to be selective for ITK over other kinases like IRK, CDK2, GSK3ß and PKA. |
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