The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.
作者信息
Bilodeau Mark T, Rodman Leonard D, McGaughey Georgia B, Coll Kathleen E, Koester Timothy J, Hoffman William F, Hungate Randall W, Kendall Richard L, McFall Rosemary C, Rickert Keith W, Rutledge Ruth Z, Thomas Kenneth A
机构信息
Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jun 7;14(11):2941-5. doi: 10.1016/j.bmcl.2004.03.052.
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.
Zotero 插件