- Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity
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The structure-activity relationships of new Aurora A/B kinase inhibitors derived from the previously identified kinase inhibitor 12 are described. Introduction of acetic acid amides onto the pyrazole of compound 12 was postulated to influence Aurora A/B selectivity and improve the profile against off-target kinases. The SAR of the acetic acid amides was explored and the effect of substitution on enzyme inhibition as well as mechanism-based cell activity was studied. Additionally, several of the more potent inhibitors were screened for their off-target kinase selectivity.
- Voss, Matthew E.,Rainka, Matthew P.,Fleming, Mike,Peterson, Lisa H.,Belanger, David B.,Siddiqui, M. Arshad,Hruza, Alan,Voigt, Johannes,Gray, Kimberly,Basso, Andrea D.
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scheme or table
p. 3544 - 3549
(2012/06/18)
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- Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors
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A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selectivity towards other kinases and desirable DMPK properties were achieved to enable the exploration of Brk as an oncology target.
- Zeng, Hongbo,Belanger, David B.,Curran, Patrick J.,Shipps Jr., Gerald W.,Miao, Hua,Bracken, Jack B.,Arshad Siddiqui,Malkowski, Michael,Wang, Yan
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p. 5870 - 5875
(2011/10/09)
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- IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS
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In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, metho
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Page/Page column 40; 41
(2009/09/05)
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- IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS
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In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions.
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