Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.

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Ducray R, Simpson I, Jung FH, Nissink JW, Kenny PW, Fitzek M, Walker GE, Ward LT, Hudson K

Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4698-701. doi: 10.1016/j.bmcl.2011.06.093. Epub 2011 Jun 29.

PubMed ID

21775140 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-[(4-Imidazo[1,2-a]Pyridin-3-Ylpyrimidin-2-Yl)Amino]Benzenesulfonamide	Cyclin-dependent kinase 2	IC 50 (nM)	1	N/A	N/A	Details