Author/Authors :
Mark T. Bilodeau، نويسنده , , Leonard D. Rodman، نويسنده , , Georgia B. McGaughey، نويسنده , , Kathleen E. Coll، نويسنده , , Timothy J. Koester، نويسنده , , William F. Hoffman، نويسنده , , Randall W. Hungate، نويسنده , , Richard L. Kendall، نويسنده , , Rosemary C. McFall، نويسنده , , Keith W. Rickert، نويسنده , , Ruth Z. Rutledge، نويسنده , , Kenneth A. Thomas، نويسنده ,
Abstract :
An azo-dye lead was modified to a novel N-(1,3-thiazol-2-yl)pyridin-2-amine series of KDR kinase inhibitors through the use of rapid analog libraries. This new class has been found to be potent, selective, and of low molecular weight. Molecular modeling has postulated an interesting conformational preference and binding mode for these compounds in the active site of the enzyme.
Keywords :
KDR kinase , VEGF.* Corresponding author. Tel.: +1-215-652-5304 , fax: +1-215-652-7310 , e-mail: mark_bilodeau@merck.com
