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Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β.
Bioorganic & Medicinal Chemistry Letters 2017 Februrary 16
The indolyl-naphthyl maleimide 7 is a potent inhibitor of the classical PKC isotypes α,β and shows excellent selectivity over the novel PKC isotypes δ,ε,η,θ and other kinases belonging to the AGC family. The SAR around 7 as well as the physico-chemical characteristics of selected derivatives and their activity in T and B cell activation and proliferation assays are discussed.
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