Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors |
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| Authors: | David B. Belanger Patrick J. Curran Alan Hruza Johannes Voigt Zhaoyang Meng Amit K. Mandal M. Arshad Siddiqui Andrea D. Basso Kimberly Gray |
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| Affiliation: | 1. Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States;2. Department of Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States;3. Department of Oncology, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States |
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| Abstract: | 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. |
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