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Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Bioorganic & medicinal chemistry letters 2010 Jul 8; In press

Link to PubMed abstract

Belanger D DB, Curran P PJ, Hruza A, Voigt J, Meng Z, Mandal A AK, Siddiqui M MA, Basso A AD, Gray K

Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States.

The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile.

Keywords: Aurora kinase