832694-16-3Relevant academic research and scientific papers
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families
Curtin, Michael L.,Frey, Robin R.,Heyman, H. Robin,Soni, Niru B.,Marcotte, Patrick A.,Pease, Lori J.,Glaser, Keith B.,Magoc, Terrance J.,Tapang, Paul,Albert, Daniel H.,Osterling, Donald J.,Olson, Amanda M.,Bouska, Jennifer J.,Guan, Zhiwen,Preusser, Lee C.,Polakowski, James S.,Stewart, Kent D.,Tse, Chris,Davidsen, Steven K.,Michaelides, Michael R.
, p. 3208 - 3212 (2012/06/18)
In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of thienopyridine ureas with promising activity against the Aurora kinases. Modification of the diphenyl urea and C7 moiety of these compounds provided potent inhibitors with good pharmacokinetic profiles that were efficacious in mouse tumor models after oral dosing. Compound 2 (ABT-348) of this series is currently undergoing Phase I clinical trials in solid and hematological cancer populations.
Thienopyridine urea inhibitors of KDR kinase
Heyman, H. Robin,Frey, Robin R.,Bousquet, Peter F.,Cunha, George A.,Moskey, Maria D.,Ahmed, Asma A.,Soni, Niru B.,Marcotte, Patrick A.,Pease, Lori J.,Glaser, Keith B.,Yates, Melinda,Bouska, Jennifer J.,Albert, Daniel H.,Black-Schaefer, Candace L.,Dandliker, Peter J.,Stewart, Kent D.,Rafferty, Paul,Davidsen, Steven K.,Michaelides, Michael R.,Curtin, Michael L.
, p. 1246 - 1249 (2007/10/03)
A series of substituted thienopyridine ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 2, are potent inhibitors of KDR (10 nM) in both enzymatic and cellular assays. Further
Thienopyridine and furopyridine kinase inhibitors
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Page/Page column 29, (2010/02/10)
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Thienopyridine and furopyridine kinase inhibitors
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, (2008/06/13)
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
