1245644-73-8Relevant articles and documents
TGF BETA RECEPTOR ANTAGONISTS
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Page/Page column 99; 101; 102, (2017/03/08)
The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβ R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors
Abraham, Sunny,Hadd, Michael J.,Tran, Lan,Vickers, Troy,Sindac, Janice,Milanov, Zdravko V.,Holladay, Mark W.,Bhagwat, Shripad S.,Hua, Helen,Ford Pulido, Julia M.,Cramer, Merryl D.,Gitnick, Dana,James, Joyce,Dao, Alan,Belli, Barbara,Armstrong, Robert C.,Treiber, Daniel K.,Liu, Gang
scheme or table, p. 5296 - 5300 (2011/10/08)
The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK profiles. Notably, compound 17l demonstrated tumor growth inhibition in a mouse xenograft model.