Discovery of N-phenyl-4-(thiazol-5-yl) pyrimidin-2-amine aurora kinase inhibitors

…, C McInnes, C Meades, M Mezna, A Plater…

文献索引：Wang, Shudong; Midgley, Carol A.; Scaerou, Frederic; Grabarek, Joanna B.; Griffiths, Gary; Jackson, Wayne; Kontopidis, George; McClue, Steven J.; McInnes, Campbell; Meades, Christopher; Mezna, Mokdad; Plater, Andy; Stuart, Iain; Thomas, Mark P.; Wood, Gavin; Clarke, Rosemary G.; Blake, David G.; Zheleva, Daniella I.; Lane, David P.; Jackson, Robert C.; Glover, David M.; Fischer, Peter M. Journal of Medicinal Chemistry, 2010 , vol. 53, # 11 p. 4367 - 4378

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被引用次数: 52

摘要

Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl) pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic histone H3 phosphorylation, and caused aberrant mitotic phenotypes. It was subsequently established that these compounds were in fact potent inhibitors of aurora A and B kinases. It was shown that potency and selectivity ...