- Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.
Bioorganic & medicinal chemistry letters (2011-07-22)
Richard Ducray, Iain Simpson, Frederic H Jung, J Willem M Nissink, Peter W Kenny, Martina Fitzek, Graeme E Walker, Lara T Ward, Kevin Hudson
PMID21775140
摘要
We disclose a novel series of insulin-like growth factor-1 receptor kinase inhibitors based on the 3-(pyrimidin-4-yl)-imidazo[1,2-a]pyridine scaffold. The influence on the inhibitory activity of substitution on the imidazopyridine and at the C5 position of the pyrimidine is discussed. In the course of this optimization, we discovered a potent and selective inhibitor with suitable pharmacokinetics for oral administration.
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