Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.
| Autor: | Ducray R; AstraZeneca, Oncology Innovative Medicines, Centre de Recherches, Z.I. Pompelle, 51689 Reims Cedex 2, France. richard.ducray@astrazeneca.com, Simpson I, Jung FH, Nissink JW, Kenny PW, Fitzek M, Walker GE, Ward LT, Hudson K |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Aug 15; Vol. 21 (16), pp. 4698-701. Date of Electronic Publication: 2011 Jun 29. |
| DOI: | 10.1016/j.bmcl.2011.06.093 |
| Abstrakt: | 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. (Copyright © 2011 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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