Title of article
Isoindolinone ureas: a novel class of KDR kinase inhibitors
Author/Authors
Michael L. Curtin، نويسنده , , Robin R. Frey، نويسنده , , H. Robin Heyman، نويسنده , , Kathy A Sarris، نويسنده , , Douglas H. Steinman، نويسنده , , James H Holmes، نويسنده , , Peter F Bousquet، نويسنده , , George A Cunha، نويسنده , , Maria D Moskey، نويسنده , , Asma A Ahmed، نويسنده , , Lori J. Pease، نويسنده , , Keith B. Glaser، نويسنده , , Kent D Stewart، نويسنده , , Steven K. Davidsen، نويسنده , , Michael R. Michaelides، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
4505
To page
4509
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 ( 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.
Keywords
KDR kinase , Isoindolinone , VEGF , Urea.* Corresponding author. Tel.: +1-847-9380463 , fax: +1-847-9355165 , e-mail: mike.curtin@abbott.com
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794821
Link To Document