Bioorganic & medicinal chemistry letters

Novel heterocycle-substituted pyrimidines as inhibitors of NF-κB transcription regulation related to TNF-α cytokine release

HH Ha, JS Kim, BM Kim

Index: Ha, Hyung-Ho; Kim, Jee Seon; Kim, B. Moon Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 2 p. 653 - 656

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Citation Number: 10

Abstract

Novel heterocyclic ring-substituted pyrimidines have been designed as inhibitors of glycogen synthase kinase-3β (GSK-3β) from the modification of known inhibitors. Several potent inhibitors exhibiting nanomolar activities were discovered against GSK-3β kinase as well as in an NF-κB reporter gene assay. Based on the results from in vitro TNF-α release inhibition and in vivo endotoxima, these inhibitors are expected to be useful candidates for ...