653600-95-4Relevant academic research and scientific papers
Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors
Fraley, Mark E.,Arrington, Kenneth L.,Hambaugh, Scott R.,Hoffman, William F.,Cunningham, April M.,Young, Mary Beth,Hungate, Randall W.,Tebben, Andrew J.,Rutledge, Ruth Z.,Kendall, Richard L.,Huckle, William R.,McFall, Rosemary C.,Coll, Kathleen E.,Thomas, Kenneth A.
, p. 2973 - 2976 (2007/10/03)
We have discovered 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as potent inhibitors of KDR kinase activity. This communication details the evolution of this novel class from a potent screening lead of vastly different structure with an emphasis on structural modifications that retained activity and provided improvements in key physical properties. The synthesis and in-depth evaluation of these inhibitors are described.
