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Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors |
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| Authors: | 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 |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. mark_fraley@merck.com |
| 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. |
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