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ID: ALA1136194
Journal: Bioorg Med Chem Lett
Title: Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.
Authors: Fraley ME, Arrington KL, Hambaugh SR, Hoffman WF, Cunningham AM, Young MB, Hungate RW, Tebben AJ, Rutledge RZ, Kendall RL, Huckle WR, McFall RC, Coll KE, Thomas KA.
Abstract: 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.
CiteXplore: 12941314