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Showing papers by "Paul Bamborough published in 2007"


Journal ArticleDOI
TL;DR: 2,4-Dianilino pyrimidines are well-known inhibitors of tyrosine kinases including lymphocyte specific kinase (Lck) and structure-activity relationships at the 4-position are discussed and rationalised.

68 citations


Journal ArticleDOI
TL;DR: In this article, a 2-amino-3,5-diarylbenzamide inhibitor of IKKα and IKK-β is described, and the most potent compounds are 8h, 8r and 8v, with IKKβ inhibitory potencies of pIC 50 7.0, 6.8 and 6.

58 citations


Journal ArticleDOI
TL;DR: In this paper, the identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole-thiophene carbonitrile inhibitors of IKK-e kinase is described.
Abstract: The identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole–thiophene carbonitrile inhibitors of IKK-e kinase is described. Compound 12e was identified with an IKK-e enzyme potency of pIC50 7.4, and has a highly encouraging wider selectivity profile, including selectivity within the IKK kinase family.