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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6739-43. doi: 10.1016/j.bmcl.2010.08.140. Epub 2010 Sep 18.

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

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, USA. david.belanger@merck.com

Abstract

We report a series of potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Optimization of the solvent accessible 8-position led to improvements in both oral bioavailability and off-target kinase inhibition. Compound 25 demonstrates anti-tumor activity in an A2780 ovarian tumor xenograft model.

PMID:
20855207
DOI:
10.1016/j.bmcl.2010.08.140
[Indexed for MEDLINE]

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