Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors.
| Autor: | Meng Z; Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States. zhaoyang.meng@merck.com, Kulkarni BA, Kerekes AD, Mandal AK, Esposite SJ, Belanger DB, Reddy PA, Basso AD, Tevar S, Gray K, Jones J, Smith EB, Doll RJ, Siddiqui MA |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 01; Vol. 21 (1), pp. 592-8. Date of Electronic Publication: 2010 Oct 12. |
| DOI: | 10.1016/j.bmcl.2010.10.008 |
| Abstrakt: | Our continued effort toward the development of the imidazo[1,2-a]pyrazine scaffold as Aurora kinase inhibitors is described. Bioisosteric approach was applied to optimize the 8-position of the core. Several new potent Aurora A/B dual inhibitors, such as 25k and 25l, were identified. (Copyright © 2010 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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