Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors
2017
Abstract As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases, such as RA, SLE, and respiratory ailments. Herein, we disclose the identification of 7-(3-(
piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]
triazin-4-amine derivatives as highly potent, selective and orally bioavailable PI3Kδ inhibitors. The
lead compounddemonstrated efficacy in an in vivo mouse KLH model.
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