Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity
Graphical abstract
Previously reported Aurora A/B inhibitor 12 was optimized to provide selectivity against a panel of off-target kinases while retaining Aurora A/B potency and good cellular activity.
Section snippets
Acknowledgments
We thank Drs. John Piwinski, Neng-Yang Shih, Paul Kirschmeier, W. Robert Bishop, Paul Zavodny and Mark Sawicki for supporting this project and the collaboration. We would also like to thank Drs. Jayaram Tagat and Tao Yu for helpful discussion on the synthesis of these compounds.
References and notes (11)
- et al.
Curr. Opin. Cell Biol.
(2003) - et al.
Expert Opin. Drug Discov.
(2011)et al.Curr. Med. Chem.
(2009)et al.Expert Opin. Investig. Drugs
(2009)et al.Expert Opin. Ther. Patents
(2009)et al.Curr. Top. Med. Chem.
(2005) - et al.
J. Med. Chem.
(2007)et al.J. Med. Chem.
(2006) - et al.
Expert Opin. Ther. Targets
(2008)et al.J. Med. Chem.
(2009) - et al.
Biochimi. Biophy. Acta, Gene Regul. Mech.
(2010)et al.Clin. Adv. Hematol. Oncol.
(2009)(c)Perez Fidalgo, J. A.; Roda, D.; Rosello, S.; Rodriguez-B., Edith; Cervantes, A. Clinical & Translational Oncology... et al.Nat. Rev. Cancer
(2007)
There are more references available in the full text version of this article.
Cited by (0)
Copyright © 2012 Published by Elsevier Ltd.