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  • Title: Isoindolinone ureas: a novel class of KDR kinase inhibitors.
    Author: Curtin ML, Frey RR, Heyman HR, Sarris KA, Steinman DH, Holmes JH, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Pease LJ, Glaser KB, Stewart KD, Davidsen SK, Michaelides MR.
    Journal: Bioorg Med Chem Lett; 2004 Sep 06; 14(17):4505-9. PubMed ID: 15357981.
    Abstract:
    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 (< 50 nM) and cellularly < or = 100 nM). 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.
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