765948-79-6Relevant articles and documents
Isoindolinone kinase inhibitors
-
Page/Page column 21, (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.
Isoindolinone ureas: A novel class of KDR kinase inhibitors
Curtin, Michael L.,Frey, Robin R.,Heyman, H. Robin,Sarris, Kathy A.,Steinman, Douglas H.,Holmes, James H.,Bousquet, Peter F.,Cunha, George A.,Moskey, Maria D.,Ahmed, Asma A.,Pease, Lori J.,Glaser, Keith B.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.
, p. 4505 - 4509 (2007/10/03)
A series of substituted isoindolinone ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 14c, are potent inhibitors of KDR both enzymatically (50nM) and cellularly (≤100nM). A 3D KDR/CDK2/MAP kinase overlay model with several structurally related tyrosine kinase inhibitors was used to predict the binding interactions of the isoindolinone ureas with the KDR active site.