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

ID: ALA1268847

Journal: Bioorg Med Chem Lett

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

Authors: Belanger DB, Williams MJ, Curran PJ, Mandal AK, Meng Z, Rainka MP, Yu T, Shih NY, Siddiqui MA, Liu M, Tevar S, Lee S, Liang L, Gray K, Yaremko B, Jones J, Smith EB, Prelusky DB, Basso AD.

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.

CiteXplore: 20855207

DOI: 10.1016/j.bmcl.2010.08.140

Patent ID: ┄